Bioactive Small Molecules

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SML1565 A-196 ≥98% (HPLC) A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. For full characterization details, please visit the A-196 probe summary on the Structural Genomics Consortium (SGC) website.

SGC2043 is the negative control for the active probe, A-196. To request a sample of the negative control from the SGC, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1410 A-366 ≥98% (HPLC) A-366 is an SGC chemical probe for G9a/GLP, developed in collaboration with Abbvie. A-366 is a potent, selective inhibitor of the histone methyltransferase G9a. The IC50 values for G9a inhbition in enzymatic and cell based assays are 3.3 and approximately 3 μM, respectively. A-366 has little or no detectable activity against a panel of 21 other methyltransferases. For full characterization details, please visit the A-366 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1923 A-395 hydrochloride ≥98% (HPLC) A-395 is a potent and selective chemical probe for the polycomb protein EED (embryonic ectoderm development), an essential component of Polycomb repressive complex 2 (PRC2), involved in transcriptional repression through methylation of histone H3K27. A-395 has been found to bind to EED in vitro with a Ki value of 0.4 nM, inhibit the PRC2 complex with an IC50 value 34 nM for methylation of H3K27, and have >100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In RD rhabdoid tumor cell line A-395 inhibited the PRC2 complex with an IC50 value of 90 nM, inhibiting the formation of H3K27me3. For characterization details of A-395, please visit the A-395 probe summary on the Structural Genomics Consortium (SGC) website.

A-395N is the negative control for the active enantiomer, A-395. A-395N is available from Sigma. To learn more about and purchase A-395N, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1033   A-278637 ≥98% A-278637 is a selective opener of ATP-sensitive K (KATP) channels (EC50 = 102 nM) that blocks contraction of bladder smooth muscle in both in vivo and in vitro assays. A-278637 is 15-fold more selective than nifedipine for bladder compared other smooth muscle KATP channels, and displays reduced effects on mean arterial pressure compared to other channel openers.
SML0595   A-286982 ≥95% (HPLC) A-286982 blocks binding of lymphocyte function-associated antigen-1 (LFA-1) with the cell adhesion molecule ICAM-1. The IC50 in a cell based assay is 35 nM.
SML1879 A-395N ≥98% (HPLC) A-395N is a control probe for A-395, which is a chemical probe for polycomb protein EED. A-395 is a potent and selective chemical probe for the polycomb protein EED (embryonic ectoderm development), an essential component of Polycomb repressive complex 2 (PRC2), involved in transcriptional repression through methylation of histone H3K27. A-395N is structurally similar, but exhibits no activity in the biochemical and cellular assays, so is an ideal control compound. For characterization details of the active probe, A-395, please visit the A-395 probe summary on the Structural Genomics Consortium (SGC) website.

A-395, the active enantiomer, is available from Sigma. To learn more about and purchase A-395, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML2192 A-485 ≥98% (HPLC) A-485 is a potent and selective catalytic inhibitor of the p300 and CREB-binding protein (CBP) histone acetyltransferases (HATs) with an IC50 value of 60 nM. A-485 was most active against haematological malignancies including most multiple myeloma cell lines as well as androgen receptor-positive prostate cancer. It was also shown to inhibit the proliferation of castration-resistant prostate cancer cells and in vivo tumour growth in SCID mice.
SML1370   A-779 trifluoroacetate salt ≥98% (HPLC) A-779 (D-Ala7-Ang-(1-7)) is a potent and selective antagonist of angiotensin (1-7), an endogenous peptide that acts through activation of a non-AT1, non-AT2 receptor, Mas, and opposes the activity of angiotensin. A-779 has an IC50 of 0.3 nM for Mas with negligible affinity for either AT1R or AT2R.
This blocking angiotensin action affects cardiovascular function.
SML0608   A-412997 dihydrochloride ≥98% (HPLC) A-412997 is a selective D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors, and no affinity for other dopamine receptors at concentrations up to 1 mM. A-412997 improves short term memory and cognitive properties in rodent models.
SML0446 A-419259 trihydrochloride ≥98% (HPLC) A-419259 is a potent inhibitor of Src family kinases. IC50 values for src, lck, blk, csk, fyn and lyn range between 15 and 50 nM.
A9736 A-438079 hydrochloride hydrate ≥98% (HPLC) A-438079 hydrochloride hydrate is a selective P2X7 purinoceptor antagonist in both human and rat with minimal activity at 75 different G-protein-coupled receptors, enzymes, transporters, and ion channels tested.
SML0861   A-484954 ≥98% (HPLC) A-484954 is a potent, selective inhibitor of eukaryotic longation factor-2 kinase (eEF2K). Eukaryotic elongation factor-2, which is required for protein synthesis, is inactivated upon phosphorylation by eEF2K.
A0862 A-740003 ≥98% (HPLC) A-740003 is a selective P2X7 purinoceptor antagonist.
SML2578 A-769662 ≥98% (HPLC) A-769662 is a potent, β1 subunit-selective, allosteric drug and metabolite (ADaM) site AMPK activator (α1β1γ1 EC50/Emax = 0.15 μM/1.99 vs. 4.51 μM/2.19 with AMP) that promotes a Thr172 phosphorylation in a β1 carbohydrate binding module (CBM) Ser108 phosphorylation-dependent manner. A769662 synergizes with AMP as well as C2 (AMP mimetic) toward Thr172 dephosphorylated/Ser108 phosphorylated AMPK. A-769662 is widely employed in probing AMPK β1 complexes-mediated cellular signaling in cultures (conc range: 1 μM-1 mM) as well as AMPK-dependent physiological and pathological processes in mice and rats in vivo (dosing range: 1-30 mg/kg i.p.).
SML2678 A-770041 ≥98% (HPLC) A-770041 is an orally available (rat F = 34.1%; 10 mg/kg p.o.), ATP-competitive, potent and selctive Lck inhibtor (IC50 = 147 nM/Lck, 1.18 μM/Lyn, 1.22 μM/Hck, 9.05 μM/Src, 14.1 μM/Fgr, 44.1 μM/Fyn; >25 μM/IKK1, IKK2, IRAK4, p38, JAK3, ZAP70, ITK, PKC, MK2, PKA, TYK2, COT,Syk; >50 μM/Tie-2 & Kdr; 1 mM ATP). A-770041 inhibits CD3 mAb-induced IL-2 production in human whole blood in vitro (IC 50 = 80 nM) and in mice in vivo (IC50 = 78 nM plasma conc.), and significantly lengthens graft survival time in a rat heterotopic heart transplant model (2.5 & 5 mg/kg bid p.o.).
SML0617   A-804598 ≥98% (HPLC) A-804598 is a P2X7 selective, competitive antagonist. In competition assays, the IC50s for human, rat and mouse channels are 11, 10 and 9 nM, respectively.
SML0818   A-841720 ≥98% (HPLC) A-841720 is a potent, selective, non-competitive mGluR1 antagonist that displays greater than 30-fold selectivity over another Group I metabotopic glutamate receptor, mGluR5. The compound has potent analgesic properties, and can also diminish motor and cognitive activity.
SML0345 A 887826 ≥98% (HPLC) A-887826 is Nav1.8 channel blocker (IC50 = 11 nM) that blocks TTX-resistant sodium currents in rat dorsal root ganglion in a voltage dependent fashion. Oral administration of A-887826 to rats significantly attenuated tactile allodynia in a neuropathic pain model.
SML0085 A-967079 ≥98% (HPLC) A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and minimal or no activity at other TRP channels or G-protein-coupled receptors, enzymes, transporters, and ion channels out of 89 tested. A-967079 blocks TRPA1 activation in human and rat cell lines and has been shown to reduce the responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons to high-intensity mechanical stimulation.
SML1744 A-971432 ≥95% (HPLC) A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist (IC50 = 6 nM/S1P5, 362 nM/S1P1 and >10 μM/S1P3 in a radio-ligand binding assay) without affect the activity of 129 protein kinases (IC50 >10 μM). A-971432 is shown to enhance blood-brain barrier integrity and reverse lipid accumulation and age-related cognitive decline in mice in vivo with good pharmacokinetics (t1/2  = 5.7 h; Cmax = 2,500 ng/ml; AUC = 35,000 ng.h/ml at 10 mg/kg, p.o. in CD1 mice). Likewise, oral gavage showed good plasma exposure and no sign of lymphopenia in rats (10, 30, and 100 mg/kg.
SML0863   A-1070722 ≥98% (HPLC) A-1070722 is a potent brain-penetrant inhibitor of glycogen synthase kinase-3 (GSK-3) α and β isoforms with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A-1070722 showed > 50-fold selectivity for GSK-3 over a panel of other kinases tested, including CDK family members. A-1070722 decreased phosphorylation of microtubule-associated protein Tau and protected rat primary cortical neurons against β amyloid and glutamate challenge.
SML1932 A-1210477 ≥98% (HPLC) A-1210477 is a BH3 mimetic that targets MCL-1 with high affinity (Ki = 0.43 nM) and selectivity (Ki >0.66 μM for BCL-2, BCL-XL, BCL-W, and A1), exhibiting little to no activity toward panels of 80 kinases (IC50 >8.5 μM) and 21 GPCRs (IC50 & EC50 >10 μM). A-1210477 selectively inhibits the survival of MCL-1-dependent (IC50 ~4 μM/multiple myeloma H929, 5.3 μM/NSCLC H2110, 7.2 μM/NSCLC H23), but not BCL-2-dependent RS4;11, cultures via apoptosis induction and potentiates BCL-2/BCL-XL inhibitor ABT-263 (Navitoclax) killing in a variety of cancer cell cultures where ABT-263 alone is ineffective. A-1210477 is also shown to cause cellular MCL-1 upregulation, most likely due to blocking MCL-1 interaction with BH3-only proteins such as NOXA and MULE known to mediate MCL-1 ubiquitylation for proteasomal degradation.
SML2121 A-33 ≥98% (HPLC) A-33 (A33) is a potent and selective catalytic site-targeting PDE4B inhibitor (IC50 = 15 nM/PDE4B vs. 1.7 μM/PDE4D) that effectively prevents PDE4B-medicated cellular cAMP hydrolysis (150%/320% increased cAMP level with 100 nM/1 μM A-33 pre-treament in murine hippocampal HT-22 cells following 10 nM isoproterenol stimulation) in vitro and inhibits LPS-induced TNF-α production in mice in vivo (ID50 = 14 mg/kg p.o.). When administered via intraperitoneal injection, A-33 improves cognitive function in a rat model of traumatic brain injury (0.3 mg/kg i.p.) and exhibits antidepressant property in mice (0.3-1 mg/kg i.p.) in vivo.
SML0788   A 83-01 ≥98% (HPLC) A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.
SML1404 A01 (Smurf1 inhibitor) ≥98% (HPLC) A01 is a high affinity selective inhibitor of E3 ubiquitin-protein ligase Smurf1 (Smad ubiquitination regulatory factor-1) that disturbs Smurf1-Smad1/5 interaction and blocks Smurf1 mediated Smad1/5 ubiquitination. A01 increases responsiveness to BMP-2 in myoblasts and osteoblasts.
A3111 A1120 ≥98% (HPLC), powder A1120 is a selective non-retinoid ligand for retinol-binding protein 4 (RBP4). RBP4 transports retinol from the liver to extrahepatic tissues and RBP4 lowering is reported to improve insulin sensitivity in mice. A1120 is a high affinity non-retinoid ligand for RBP4 which disrupts the interaction between RBP4 and its binding partner transthyretin (TTR). It binds to the same site as retinol and induces changes in the orientation (compared to the retinol bound form) of loops at the RBP4-TTR interaction interface.A1120 lowers RBP4 and retinol levels in a dose-dependent manner, to a similar extent as seen with fenretinide. However, unlike fenretinide (Sigma# H7779), A1120 does not have beneficial effects on insulin resistance.
A8736 A12B4C3 ≥98% (HPLC) A12B4C3 is a potent and specific hPNKP phosphatase inhibitor. A12B4C3 doubles the radiosensitivity of human A549 lung carcinoma and MDA-MB-231 breast adenocarcinoma cells.
A2846 A-134974 dihydrochloride hydrate ≥98% (HPLC), solid A-134974 is a novel and selective adenosine kinase (AK) inhibitor with IC50 = 60 pM. Systemic A-134974 (i.p.) dose dependently reduced hyperalgesia (ED50= 1 μmol/kg) and at higher doses, reduced locomotor activity (ED50 = 16 μmol/kg). Administration of A-134974 intrathecally (i.t.) was more potent (ED50= 6 nmol) at producing antihyperalgesia than delivering the compound by intracerebralventricular (ED50 = 100 nmol, i.c.v.) or intraplantar (ED50 >300 nmol) routes. In contrast, i.c.v. administration of A-134974 was more effective in reducing locomotor activity than i.t. administration (ED50 values were 1 and >100 nmol, respectively). Increasing the pretreatment time for i.t.-delivered A-134974 caused a greater reduction in locomotor activity (ED50= 10 nmol). This was due to diffusion of A-134974 (i.t.) to supraspinal sites. These data demonstrate that the novel AK inhibitor A-134974 potently reduces thermal hyperalgesia primarily through interactions with spinal sites, whereas its ability to depress locomotor activity is predominantly mediated by supraspinal sites.
SML2277 A192621 ≥98 (HPLC) A192621 is a selective; orally available ETB endothelin receptor antagonist. A192621 has been shown to cause an increase in arterial blood pressure and to promote apoptosis in human pulmonary arterial smooth muscle cells.
SML0471 A22 hydrochloride ≥95% (HPLC) A22 is an inhibitor of MreB, an actin-like bacterial protein, and has been shown to act as an antiobiotic adjuvant. A22 inhibition of MreB disrupts the bacterial actin cytoskeleton, which can cause an increase in cell permeability and altered transport. A22 has been shown to have synergistic effects with several antibiotics including novobiocin and rifampin in gram negative bacteria.
A1980 A3 hydrochloride ≥98% (HPLC), solid Non-selective casein kinase (CK) inhibitor. A shorter alkyl chain derivative of W-7 that inhibits casein kinase I (Ki = 80 μM), casein kinase II (Ki = 5.1 μM), myosin light chain kinase (Ki = 7.4 μM), protein kinase A (Ki = 4.3 μM), protein kinase C (Ki= 47 μM), and protein kinase G (Ki = 3.8 μM).
A2979 A-317491 sodium salt hydrate ≥98% (HPLC), powder A-317491 helps to decrease neuropathic and inflammatory pain by inhibiting the P2X3 receptor-mediated Ca2+ influx.
Novel P2X3 and P2X2/3 receptor antagonist
A7730 A-331440 dihydrochloride ≥98% (HPLC), solid A-331440 dihydrochloride is a non-imidazole H3 histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate release of histamine and other neurotransmitters, and histamine H(3) receptor antagonists enhance neurotransmitter release. A-331440 is a histamine H(3) receptor antagonist, which binds potently and selectively to both human and rat histamine H(3) receptors (K(i)=25 nM). Mice on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. Both data shows that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent.
A3104 A-331440 L-tartrate hydrate ≥98% (HPLC), solid Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H3 receptors regulate release of histamine and other neurotransmitters, and histamine H3 receptor antagonists enhance neurotransmitter release. A-331440 [4′-[3-(3(R)-(dimethylami<WBR>no)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile] is a histamine H3 receptor antagonist which binds potently and selectively to both human and rat histamine H3 receptors (Ki<=25 nM). Mice were stabilized on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H3 receptor antagonist, A-331440, has potential as an antiobesity agent.
A6604 A-350619 hydrochloride ≥98% (HPLC), solid A-350619 modulates catalytic properties of soluble guanylyl cyclase; it increases Vmas from 0.1 to 14.5 μmol/min/mg and lowers Km from 300 to 50 μM. A-350619 activation of soluble guanylate cyclase depends on the presence of a heme moiety in the enzyme and synergy with nitric oxide.
SML1731 A64 trifluoroacetate ≥98% (HPLC) A64 is a cell-permeable, ATP site-targeting pyridone thiazolidinedione compound that acts as a potent HIPK2-selective homeodomain-interacting protein kinase inhibitor (IC50 = 74 nM and 136 nM against HIPK2 and HIPK1, respectively; [ATP] = 100 μM), affecting MPF only at higher concentrations (by 35% at 5 μM; [ATP] = 10 μM) and exhibiting little potency toward CDK1 (IC50 >10 μM). A64 (1 μM) effectively prevents ER stresser tunicamycin (1 μg/mL) -induced HIPK2/JNK phosphorylation and cell death in HEK293 and primary rat motor neuron cultures. HIPK2 inhibition by A64 treatment is also efficacious in protecting rat motor neurons from death upon exogenous SOD1 G93A or TDP-43 expression. ff-target kinases revealed by kinome profiling include DYRK1A, CSNK2A2, DAPK2, DAPK1, PIM3, CSNK2A1, PIM1 (Kd = 8.8, 6.1, 6.1, 9.5, 3.7, 31, 37 nM, respectively) and DYRK1B (IC50 = 62 nM).
SML1213 A66 ≥98% (HPLC) A66 is a potent and highly selective inhibitor of the phosphoinositide 3-kinase (PI3K) catalytic subunit p110α with an IC50 of 32 nM and >100 fold selectivity for p110α over other class-I PI3K isoforms.
SML2908   A71915 trifluoroacetate ≥95% (HPLC) New A71915 is a potent atrial natriuretic peptide A (ANP, NPPA) receptor (NPR1, ANP-A, ANPR-A, NPR-A) antagonist (pKi = 9.18 (Ki = 650 nM) by competitive binding against 300 nM rat ANP1-28 to human neuroblastoma NB-OK-1 cells; pA2 = 9.45 against rat ANP-induced cGMP production in NB-OK-1 cells). A71915 is reactive toward dog, human, mouse, rabbit, and rat species, and commonly employed both in cultures (1-10 μM) and in vivo for studying NPR-A-mediated responses.
A255 A-77636 hydrochloride hydrate ≥98% (HPLC), solid Potent, orally active D1 dopamine receptor agonist.
human ... DRD1(1812)
A3109 A-803467 ≥98% (HPLC) A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
SML2356 A939572 ≥98% (HPLC) A939572 is an orally available piperidine-aryl urea-based small molecule that inhibits stearoyl-CoA desaturase 1 (SCD1) with high potency (IC50 = 37 nM/hSCD1 and <4 nM/mSCD1) with little hERG channel blockade activity (IC50 >100 μM). When administered in ob/ob mice, A939572 effectively reduces desaturation indices in vivo (18:0/18:1n9 ratio from 26.9 to 8.47 in liver; from 15.4 to 7.35 in plasma post 5-day 10 mg/kg bid p.o.). A939572 is a useful tool for probing SCD1-mediated physiological and pathological processes both in cultures (50 nM-10 μM) and in vivo (5-10 mg/kg i.p. or 10 mg/kg p.o. in mice).
SML0266 AA 29504 ≥98% (HPLC) AA29504 is a GABAA positive modulator with a preference for extra-synaptic α4β3δ over α1β3γ2s synaptic receptors. AA29504 exhibits anxiolytic effects and reduces motor coordination in rat models.
SML0358 AA74-1 ≥98% (HPLC) AA74-1 is an extremely potent and selective inhibitor of the serine hydrolase acyl-peptide hydrolase (APEH) with an IC50 of 5 nM in mouse T-cell proteomes. AA74-1 potently blocked the activity of its target serine hydrolase, APEH, in mice in vivo without significantly affecting other enzymes. The APEH inhibition caused accumulation of N-acetylated proteins and stimulated cellular proliferation in T cells.

The APEH gene is deleted in some cancers, in which it has been proposed to serve as a potential tumor suppressor, and is involved in the degradation of oligomeric amyloid-beta which could make it a new target for therapy aimed at reducing neurodegeneration in Alzheimer′s disease. AA74-1 is the first selective tool for studying APEH activity.
SML0865   AA92593 ≥98% (HPLC) AA92593 blocks melanopsin activity and stimulates α-melanocyte-stimulating hormone (α-MSH) expression and induces melanin distribution in the melanophores, which darkens the embryo.
AA92593 is an opsinamide, a potent antagonist of melanopsin-mediated phototransduction with an IC50 of 665 nM in a Ca2+ flux assay in CHO cells expressing melanopsin (Opn4) and selectivity > 10 μM at 74 common biological targets. AA41612 is believed to act by competing for binding to melanopsin. AA41612 inhibited mouse pupillary light reflex and light aversion in vivo. AA92593 and similar compounds might be useful in alleviating the photophobia associated with migraine.
SML1761 AA-CW236 ≥98% (HPLC) AA-CW236 is a cell-permeable chloromethyl triazole (CMT) derivative that acts as a non-pseudosubstrate inhibitor against human O(6)-alkylguanine DNA methyltransferase (MGMT) by targeting MGMT active site Cys145 for covalent modification (KI = 24 nM, kinact = 0.03/min), displaying little affinity toward cysteines from other cellular proteins. AA-CW236 pretreatment (1 μM) effectively prevents MGMT from repairing DNA damage, causing significantly more upregulated O6-alkylguanine accumulation than the pseudosubstrate inhibitor Lomeguatrib (1 μM) when co-administered with the DNA-alkylating agent Temozolomide/TMZ (300 μM) in MCF-7 cells. Likewise, AA-CW236 is shown to boost TMZ toxicity in Caco-2 cultures (IC50 = 227 and 673 μM, respectively, with or without 3 μM AA-CW236 co-treatment).
UC432 AAMU    
A4111   2-AAPA hydrate ≥95% (HPLC) Abnormal thiol redox state (TRS) is involved in the pathogenesis of a variety of diseases, such as chronic heart disease and atherosclerosis, rheumatoid arthritis , AIDS , Parkinson disease, Alzheimer disease, etc. Thus there is a need for tools capable of regulating TRS. Glutathione reductase (GR) is a critical enzyme in the homeostasis of TRS. Thus selective GR inhibitor would be a valuable research tool in studying TRS-related processes. Carmustine (#C0400) an anticancer drug is commonly used as GR inhibitor (IC50~470 microM). 2-AAPA is novel, potent cell-penetrable GR inhibitor. The compound is quite selective. But small reduction of activity for GP and GST was observed at 0.1mM concentration of 2-AAPT.
Glutathione reductase (GR) is a critical enzyme in the homeostasis of cellular thiol redox state. 2-AAPA is potent, selective, cell-permeable GR inhibitor, a valuable research tool in studying processes related to thiol redox state. For example, it was used in a study of the relationship between thiol redox state and overall redox state. In addition to the expected decrease in GSH and increase in GSSG, 2-AAPA increased the ratios of NAD(P)H/NAD(P)+. Significant protein glutathionylation was also observed.
SML2859 AB-1 ≥98% (HPLC) New AB-1 is a highly selective estrogen receptors ERα and ERβ modulator over G protein-coupled estrogen receptor GPER. AB-1 is an agonist of ER transcriptional activity, but it acts as an antagonist of rapid signaling through ERα.
highly selective estrogen receptors ERα and ERβ modulator over G protein-coupled estrogen receptor GPER
SML0089 Abacavir sulfate ≥98% (HPLC) Abacavir incorporated in the cells is converted to triphosphate containing guanine analog carbovir (CBV) and it favors the generation of higher double stranded breaks (DSBs).
Abacavir sulfate is a Nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
SML2919   Abarelix acetate New Abarelix (PPI-149) is a gonadotropin releasing hormone (GnRH)/luteinizing hormone releasing hormone (LHRH) receptor (GnRHR, LHRHR) antagonist with low histamine release induction propensity (EC50 = 100 μg/mL; rat mast cells). Abarelix exhibits good in vivo efficacy via iv. or sc. in suppressing LH levels in castrated male rats (plasma LH = 12/1.2/0.9/1.2 ng/mL 6 hrs post 0/12.5/50/200 μg/kg in 5% mannitol sc.) and in lowering testosterone among intact male rats (plasma testosterone = 1.64/0.29 ng/mL 6 hrs post 0/3 μg/kg sc.).
SML2622 ABC1183 ≥98% (HPLC) ABC1183 is an orally active, potent and selective inhibitor of GSK3 α/β and CDK9, which induces G2/M cell cycle arrest and apoptosis in cancer cells. Apparently ABC1183 suppresses tumor growth and inflammation-driven gastrointestinal disease symptoms due to down regulation of TNFα and IL-6 pro-inflammatory cytokines. It does not exhibit organ or hematological toxicities.
SML1816 ABC44 ≥98% (HPLC) ABC44 is a cell-active, potent and selective inhibitor of palmitoyl-protein thioesterase 1 (PPT-1).
SML2410 ABC99 ≥98% (HPLC) ABC99 is an N-hydroxyhydantoin (NHH) carbamate-based irreversible, potent and selective inhibitor against the serine hydrolase activity of the Wnt-deacylating enzyme NOTUM (IC50 = 13 nM against NOTUM-mediated labeling of fluorophosphonate (FP) probe), an enzyme that reverses the posttranslational O-linked palmitoleate modification of Wnt proteins. ABC99 prevents NOTUM-mediated negative regulation against Wnt3A-dependent cellular signaling (EC50 = 89 nM by HEK293T TOPflash reporter assay) with excellent selectivity over 65 other serine hydrolases, including PPT1.
Inhibition of NOTUM has therapeutic use in treating degenerative diseases including osteopenia and osteoporosis.
SML1466 ABH hydrochloride ≥98% (HPLC) ABH (2(S)-amino-6-boronohexanoic acid) is a highly potent and specific arginase inhibitor that inhibits the LPS-induced increases in pulmonary IL-8, neutrophils and goblet cells as well as airway fibrosis in rodent model of COPD.
Selective inhibition of arginase by ABH in animal models is known to ameliorate the effect of diabetes mellitus type 1, autoimmune encephalitis, chronic asthma and vascular stiffness due to aging. ABH inhibition of arginase restores erectile hemodynamics in aging mouse. Ex vivo studies prove that ABH promotes smooth muscle relaxation stimulated by nitric oxide.
SML1527 Abiraterone acetate ≥98% (HPLC) Abiraterone acetate is a prodrug of abiraterone, which is a potent, selective, and orally bioavailable inhibitor of CYP17A1 (CYP450c17), an enzyme that catalyzes two key serial reactions (17α hydroxylase and 17,20 lyase) in androgen and estrogen biosynthesis resulting in the formation of DHEA and androstenedione, which may ultimately be metabolized into testosterone. CYP17 is the key enzyme for androgen biosynthesis in both the testes and adrenals, so its inhibition should stop the production of androgens in both places. Abiraterone acetate is used for the treatment of metastatic castration-resistant prostate cancer. Abiraterone acetate possesses significant antitumor activity in post-docetaxel patients with CRPC (castration-resistant prostate cancer). It is highly essential for androgen biosynthesis in the testes, adrenal glands, and prostate tissue.
human ... CYP17A1(1586)
SML1963   Abiraterone D4A metabolite ≥98% (HPLC) D4A (Δ4-Abiraterone; 3-Pyridinyl)-androsta-4,16-dien-3-one) is an abiraterone metabolite found to be more active than abiraterone. Abiraterone is a potent, selective, and orally bioavailable inhibitor of CYP17A1 (CYP450c17), an enzyme that catalyzes two key serial reactions (17 alpha hydroxylase and 17,20 lyase) in androgen and estrogen biosynthesis resulting in the formation of DHEA and androstenedione, which may ultimately be metabolized into testosterone. CYP17 is the key enzyme for androgen biosynthesis in both the testes and adrenals, so its inhibition can stop the production of androgens in both places. It is approved for the treatment of metastatic castration-resistant prostate cancer. D4A blocks not only CYP17A1, but also blocks two other enzymes, 3?-hydroxysteroid dehydrogenase (3?HSD) and steroid-5?-reductase (SRD5A), which are involved in producing the androgen 5?-dihydrotestosterone (DHT), while also blocking the androgen receptor.
SML0294 ABL127 ≥98% (HPLC) ABL127 is a potent and selective inhibitor of Protein phosphatase methylesterase-1 (PME-1 or PPME-1). IC50 values were 11.1 nM and 6.4 nM in MDA-MB-231 and HEK 293T cells with no activity detected against >50 other serine hydrolases. PME-1 regulates the methylesterification state of protein phosphatase 2A (PP2A) and is implicated in cancer and neurodegeneration.
A236 AB-MECA solid High affinity A3 adenosine receptor agonist.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
I145 I-AB-MECA solid Reference standard for radioiodinated I-AB-MECA, a widely used, high affinity radioligand for the A3 adenosine receptor.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
SML0904   ABO dihydrochloride ≥98% (HPLC) ABO is a modulator of Annexin A7 (ANXA7) GTPase, a member of the annexin family of calcium/phospholipid-binding proteins. ABO can directly bind to Annexin A7 and inhibit its phosphorylation. Annexin A7 is involved in several processes especially in the process of membrane fusion and exocytosis. ABO is a GTPase, and both GTP-binding and Protein kinase C (PKC) activity are important in regulating its function to potentiate calcium-dependent membrane fusion. Annexin A7 has several other activities, not fully understood. ABO suppressed oxidized low-density lipoprotein (oxLDL)-induced phosphatidylcholine-specific phospholipase C (PC-PLC) activity, inhibiting apoptosis and promoting autophagy in vascular endothelial cells, indicating that ANXA7 is an endogenous regulator of phosphatidylcholine-specific phospholipase C (PC-PLC). ABO significantly reduced atherosclerotic plaque area and reduced lipid deposition and pro-inflammatory macrophages in apolipoprotein E-/- mice. ABO should be a valuable tool to study the complex functions of Annexin 7.
A8451 (−)-cis,trans-Abscisic acid    
A4906 (+)-Abscisic acid ≥98% (HPLC) Plant hormone and growth regulator that is involved in several physiological mechanisms including seed dormancy, leaf abscission, stomatal movement, and plant stress responses. Through complex interactions with several intracellular signaling systems, it can regulate the expression of hundreds of plant genes.
A6476 ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
A9227 ABT-491 hydrochloride ≥98% (HPLC) Highly potent, selective and orally active platelet-activating factor (PAF) receptor antagonist. Ki = 0.6 nM in human platelets.
A5111 ABT-724 trihydrochloride ≥98% (HPLC)    
SML0131 ABT-751 hydrochloride ≥98% (HPLC) ABT-751 is an orally bioavailable vascular disrupting agaent (VDA) with a broad spectrum of antitumor activity. It binds to the colchicine binding site on beta-tubulin and inhibits polymerization of microtubules.
A4980   Abz-FRK(Dnp)P-OH trifluoroacetate salt ≥95% (HPLC), film Substrate for ACE (Angiotensin Converting Enzyme). Internally quenched fluorogenic substrate for Real Time Fluorescent Assay.
A5855 Abz-LFK(Dnp)-OH trifluoroacetate salt ≥97% (HPLC) Abz-LFK(Dnp)-OH is an Angiotensin Converting Enzyme (ACE) fluorescent peptide substrate specific for the C domain for real time fluorescent assay (ACE, Peptidyl Dipeptidase, Kininase II, E.C.
A5730 Abz-SDK(Dnp)P-OH trifluoroacetate salt ≥91% (HPLC), lyophilized powder Abz-SDK(Dnp)P-OH is an Angiotensin Converting Enzyme (ACE) fluorescent peptide substrate specific for the N domain for real time fluorescent assay (ACE, Peptidyl Dipeptidase, Kininase II, E.C.
SML0787   AC 42 ≥98% (HPLC) AC-42 is a specific agonist of the muscarininc M1 receptor (pEC50 = 6.54) with little or no activity against other muscarinic receptor family members. AC-42 binds to an allosteric site adjacent to the adjacent to the orthosteric, acetylcholine binding site.
SML1418   AC187 trifluoroacetate salt ≥95% (HPLC) AC187 is an orally active, potent and selective amylin receptor antagonist that increases glucagon secretion, alters plasma glucose levels and increases food intake in vivo. AC187 completely blocks internalization of amylin monomers in pancreatic cells. AC187 blocks β-amyloid neurotoxicity in rats.
SML2244 AC1903 ≥98% (HPLC) AC1903 is a specific inhibitor of TRPC5, the transient receptor potential canonical channel 5, a Ca2+ permeable nonselective cation channel highly expressed in brain and kidney. AC1903 did not inhibit TRPC4 or TRPC6 currents and showed no off-target effects in kinase profiling assays. It specifically blocked TRPC5 channel activity in glomeruli of proteinuric rats, suppressed severe proteinuria, showing a therapeutic benefit in a rat model of hypertensive proteinuric kidney disease.
SML0625   AC253 trifluoroacetate salt ≥95% (HPLC) AC253 is an antagonist of Amylin, one of the peptides in the Calcitonin-gene related peptide (CGRP) family. In recent studies. AC253 restored memories in brain cells taken from animals used as models of Alzheimer′s disease. Application of AC253 significantly enhanced long-term potentiation (LTP) when given to 6- to 12-month-old TgCRND8 mice that normally show blunted LTP. In other studies, AC25 neutralized the depressant effects of Aβ(1-42) on hippocampal LTP without affecting baseline transmission or LTP on its own.
SML2667 AC261066 ≥98% (HPLC) AC261066 is an orally active, selective and potent synthetic agonist for the retinoic acid β2-receptor (RARβ2) that decreases oxidative stress in mice fed a high-fat diet. AC261066 reduce ischemia/reperfusion injury of the heart in mice models.
SML0129 AC-265347 ≥98% (HPLC) AC-265347 is a calcimimetic that acts as agonist to calcium-sensing receptor. It reduces serum parathyroid hormone and plasma ionizable calcium.
AC-265347 is a human calcium-sensing receptor (CaSR) allosteric agonist. AC-265347 activates CaSR signaling in cellular proliferation and phosphatidyl inositol (PI) hydrolysis assays.
A7980 AC-41848 hydrate ≥98% (HPLC), solid AC-41848 is a potent, cell permeable, subtype selective retinoic acid receptor RARγ agonist. AC-41848 has high selectivity (92%) for RARγ. EC50 = 5.9 μM.
A3609 AC-55541 ≥98% (HPLC), powder    
A0355 AC-7954 ≥98% (HPLC), solid Nonpeptide GPR14 / urotensin-UII (UII) receptor agonist that has an EC50 of 300 nM at the human UII receptor (h-UTR). AC-7954 has been shown to exist in two conformations, A and B; both conformations have a pharmacophoric distance within 0.5 Å of P5U, a potent peptidic UII agonist.
human ... UTS2R(2837)
A9605 AC-93253 iodide ≥98% (HPLC) AC-93253 is a potent, cell permeable, subtype selective RAR (RARα) agonist. EC50 = 6.3 μM. AC-93253 has high selectivity; 89% for RARα vs 67% for RARβ1, 35% for RARβ2, and 11% for RARγ.
A6981 Acamprosate calcium ≥98% (HPLC), powder Acamprosate calcium is a GABA γ-aminobutyric acid agonist.
Acamprosate calcium is a synthetic analog of γ-aminobutyric acid (GABA) and a GABAB receptor agonist. Acamprosate calcium has been used in alcohol dependence treatments and may be an effective augmentation therapy anxiety patients.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879), GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRIN3A(116443), GRIN3B(116444)
A9354   Ac-Arg-Glu(EDANS)-Val-His-His-Gln-Lys-Leu-Val-Phe-Lys(DABCYL)-Arg-OH trifluoroacetate salt ≥95% (HPLC), powder α-Secretase substrate II, fluorogenic.
5.30616 ACE2 Inhibitor, MLN-4760 ≥97% (HPLC), powder, Calbiochem® MLN-4760 is bioavailable and exhibits far greater selectivity for carboxypeptidase (IC50 = 0.44 nM against 50 pM human ACE2; [ZnCl2] = 10 μM, [MCA-APK(DNP)] = 50 μM) over bovine carboxypeptidase A or ACE peptidyldipeptidase activity (IC50 = 27 μM and >100 μM against 0.5 nM bovine CPDA and 1 nM porcine ACE, respectively; [Substrate] = 50 μM) and porcine ACE (IC50 = 27 and >100 μM, respectively). This reversible ACE2 inhibitor binds to the active site zinc with high-affinity and emulates the transition state during peptide hydrolysis. It reduces serum and kidney ACE 2 activity and abolishes angiotensin II-induced hypertension in mice. MLN-4760 selectively blocks angiotensin (ANG-(1-7)) formation in ACE2 wild type (WT) mice subjected to low ANG II concentrations (<0.1 μM), but at higher ANG II concentrations it does not affect ANG -(1-7) levels in mice. This ACE2 inhibitor enhances tumor necrosis factor (TNF) (10 pg/mL) stimulated expression of proinflammatory cytokines in murine endothelial cells, (1 μM using SVEC-40 line and primary aorta endothelial cultures) in vitro. MLN-4760 is widely employed for studying ACE2 involvement in kidney, cardiovascular and inflammatory bowel diseases via drinking water (10 mg/kg/d), i.v. (0.1 mg/kg), and s.c. (30 mg/kg/d to 300 mg/kg/12 h) injection in rats and mice, in vivo. The inhibitor leucine moiety is shown to simultaneously target ACE2 substrate S1 pocket with its isobutyl group and active site zinc via its carboxylate, while the compound′s 3,5-dichlorobenzyl group effectively occupy S1′ subsite.
MLN-4760 also enables to study the effect of reduced ACE2 activity on the lung’s susceptibility for Coronavirus disease (COVID) related acute respiratory distress syndrome (ARDS).
SML0180 Aceclidine hydrochloride ≥98% (HPLC) Aceclidine at a concentration of 5 and 50 μg is capable of enhancing the outflow facility, following ciliary muscle disinsertion.
Aceclidine hydrochloride is a parasympathomimetic drug with weak anticholinesterase activity. It acts on cholinergic nerve-endings, lowers intraocular pressure and potent therapeutic agent for open-angle glaucoma.
Aceclidine is a non-selective muscarinic acetylcholine receptor partial agonist that is effective in reducing intraocular pressure.
A8861 Aceclofenac ≥98% (HPLC) Non-steroidal, anti-inflammatory drug (NSAID), with selectivity for COX-2 over COX-1.
human ... PTGS2(5743)
SML0395 Ac-EEMQRR-NH2 trifluoroacetate salt ≥95% (HPLC) Ac-EEMQRR-NH2 is a SNAP25 N-terminal-derived peptide that inhibits the SNARE complex and possibly blocks neuronal exocytosis. Ac-EEMQRR-NH2 exhibits anti-inflammatory and anti-wrinkle activity. It is used as anti-wrinkle cosmetics ingredient.
Ac-EEMQRR-NH2 trifluoroacetate salt is considered 4000 times less toxic than botulin toxin. It has restricted transdermal penetration and hence has limited application for topical usage.
A201 Acenaphthenequinone    
SML0074 Acenocoumarol ≥98% (HPLC) Acenocoumarol is a warfarin analog, an anticoagulant that inhibits Vitamin K epoxide reductase. This results in depletion of the reduced form of vitamin K (vitamin KH2), limiting the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S, resulting in decreased prothrombin levels and the amount of thrombin generated.
Acenocoumarol is effective against thromboembolic disorders.
human ... VKORC1(79001)
A7111 Acepromazine maleate ≥98% (HPLC) Acepromazine is a phenothiazine antipsychotic comonly used as a veterinary drug (horses, dogs and cats). The compound is an analogue antipsychotic drug chlorpromazine (#C8138). The drug is thought to block receptors of dopamine in the brain. Recently it was discover that the compound inhibits ABCG2 transported protein, which overexpression in tumors is associated with drug resistance.
A3750 21-Acetoxypregnenolone    
P7568 β-Acetyl-γ-O-alkyl-L-α-phosphatidylcholine from bovine heart lecithin ≥99%, lyophilized powder Phospholipid produced by lymphocytes, platelets and endothelial cells that induces platelet aggregation and is involved in inflammation, anaphylaxis and wound repair.
A9598   N-Acetyl-Asp-Glu-His-Asp-7-amido-4-methylcoumarin trifluoroacetate salt ≥95% (HPLC)    
A1086 N-Acetyl-Asp-Glu-Val-Asp-7-amido-4-methylcoumarin ≥97% (HPLC), powder Fluorogenic substrate for caspase 3, a protease that is rapidly activated when cells are exposed to apoptotic conditions and that cleaves poly(ADP-ribose) polymerase.
A0737 N-acetylcysteine amide ≥98% (HPLC) N-acetylcysteine amide is a membrane penetrating antioxidant with antiinflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS. The compound readily crosses cell membranes, replenishes intracellular GSH, and defends the cell from oxidative stress. In contrast to DTT, AD4 is able to directly reduce intracellularl GSSG to GSH without the involvement of glutathione peroxidase. Such direct thiol exchange might have a protective effect. This compound has a potential in research and exploration for treatment of neurodegeneration, radiation exposure, and other oxidation-mediated disorders.
A6166 3-Acetyldeoxynivalenol from Fusarium roseum    
A1556 15-O-Acetyl-4-deoxynivalenol from Fusarium graminearum    
C001 Acetylethylcholine mustard hydrochloride >97% (GC), powder Acetylethylcholine mustard is a precursor for ethylcholine mustard aziridinium ion (AF-64A); irreversible ligand for the high affinity choline transport system; specific presynaptic long action cholinotoxin; inhibitor of choline acetyl-transferase.
SML1017   Acetyl fentanyl ≥98% (HPLC) Acetyl fentanyl is an impurity formed in the production process of fentany, and is a very potent μ opiod receptor agonist.
A1341 N-Acetyl-Glu-Ser-Met-Asp-al ≥90% (HPLC), powder In the caspase-3 precursor, procaspase-3, the ESMD amino acid sequence has been identified as a cleavage site for producing the p17 and p12 subunits of mature caspase 3; Ac-ESMD-CHO has been shown to inhibit the protease that cleaves procaspase-3 at this site. Ac-ESMD-CHO binds caspase-7 and inhibits with a Ki of approximately 1300 nM, which makes it a weaker inhibitor than other inhibitor tetrapeptide analogs.
P4904 β-Acetyl-γ-O-hexadecyl-L-α-phosphatidylcholine hydrate ≥98% Extracellular signaling lipid; ligand for G protein-coupled platelet activating factor (PAF) receptors. Induces inflammation by increasing vascular permeability; activates MAP kinase (MAPK) and MAP kinase kinase (MAPKK) in CHO cells.
A5720 N-Acetyl-Leu-Glu-Glu-Asp-7-amido-4-trifluoromethylcoumarin ≥90% (HPLC), powder    
A5513 N-Acetylprocainamide hydrochloride ≥99% (HPLC), powder N-acetyltransferase II in liver catalyzes the conversion of procainamide to N-acetylprocainamide (NAPA).
Class III antiarrhythmic. Increases the duration of the action potential by decreasing the delayed outward potassium current, slightly decreasing the calcium current, and slightly depressing the inward rectifier potassium current. This is the active metabolite of procainamide that does not induce systemic lupus erythematosus.
A7191 N-Acetyl-D-sphingosine ≥97% (TLC), powder Cell-permeable, biologically active ceramide. It induces differentiation and apoptosis in cells and has been shown to activate protein phosphatases.
A6720 N-Acetyl-Trp-Glu-His-Asp-7-amido-4-trifluoromethylcoumarin trifluoroacetate salt ≥97% (HPLC), powder Fluorogenic substrate for caspase 1 and 5.
A4339   N-Acetyl-Tyr-Val-Lys(biotinyl)-Asp 2,6-dimethylbenzoyloxymethyl ketone ≥90% (HPLC), powder    
SML0357 AcH4-21 trifluoroacetate salt ≥95% (HPLC) AcH4-21 is a good substrate of Protein Arginine Methyltransferases (PRMTs).
SML2868   Aclidinium bromide ≥98% (HPLC) New Aclidinium bromide is a long-acting muscarinic antagonist (LAMA) bronchodilator. It is a muscarinic M3, M2 antagonist with a long residence time at M3 receptors and a shorter residence time at M2 receptors. Aclidinium bromide was approved for the treatment of chronic obstructive pulmonary disease (COPD) in July 2012.
A9229 Ac-Lys-(Me)Leu-Val-(Me)Phe-Phe-NH2 trifluoroacetate salt ≥95% (HPLC) Amyloid β40 fibrillogenesis inhibitor
A8001 Aconitine ≥95% (HPLC), crystalline Neurotoxin. Activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction. Aconitine also blocks norepinephrine reuptake. In the heart, aconitine induces ventricular tachycardia after intracoronary injection. In cultured ventricular myocytes, aconitine increases the duration of the action potential and induces the appearance of early after depolarization.
SML1569 Acotiamide dihydrochloride ≥98% (HPLC) Acotiamide is a potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE). Acotiamide showed no affinity for dopamine D2 or serotonin 5-HT4 receptors but does have activity as a muscarinic antagonist. It acts as a prokinetic drug through acetylcholinesterase inhibition and muscarinic receptor antagonism, and has been used for the treatment of functional dyspepsia (FD) involving gastric motility dysfunction.
A2112 Ac-PGP trifluoroacetate salt hydrate ≥98% (HPLC) N-acetyl Proline-Glycine-Proline (ac-PGP) is a potent and selective neutrophil chemoattractant. It is generated enzymatically from extracellular matrix proteins such as collagen. PGP is generated from native collagen by the action of matrix metalloproteinase–8 (MMP-8) and/or MMP-9, followed by a secondary cleavage by prolyl endopeptidase (PE). N-terminal acetylation of PGP (Ac-PGP) occurs through an unknown mechanism. Both PGP and AcPGP are considered biomarkers and possible therapeutic targets for chronic obstructive pulmonary disease (COPD) and may also be markers for acute pulmonary exacerbation in Cystic Fibrosis.
SML0119 Acrivastine ≥98% (HPLC) Acrivastine is a second-generation antihistamine, an H1-receptor antagonist.
Acrivastine is a second-generation antihistamine. It is a derivative of first-generation compound triprolidine. Acrivastine is effectively used for treating allergic diseases including cholinergic urticaria and histamine-medicated dermatoses.
human ... HRH1(3269)
SML2885   Ac-SDKP trifluoroacetate ≥95% (HPLC) Originally characterized as a "spleen colony-forming units (CFU-S) inhibitor" for its activity against hematopoietic pluripotent stem cell proliferation, Ac-SDKP (Goralatide) is an immunomodulatory and pro-angiogenic tetrapeptide derived from the N-terminal end of thymosin β4 (Tβ4 aa 1-4) via sequential enzymatic actions of meprin-α and prolyl-oligopeptidase (POP), while angiotensin converting enzyme (ACE) mediates Ac-SDKP degradation. In animal heart, kidney and brain injury studies, Ac-SDKP ameliorates end-organ damage by promoting angiogenesis, as well as by reducing inflammation and fibrosis.
SML1393 ACT-462206 ≥98% (HPLC) ACT-462206 is a orally active, brain penetrant, potent and selective dual orexin1/2 receptor antagonist (DORA). ACT-462206 decreases wakefulness, decreases sleep latency, and increases sleep efficacy in rats and dogs.
A6671 Actinonin Actinonin has inhibitory action against peptide deformylase (PDF). It is effective against Gram-positive and fastidious Gram-negative microorganisms.
Actinonin is an inhibitor of leucine aminopeptidase. Actinonin has also been used to improve antibacterial activity and antiobesity therapeutics.
human ... ANPEP(290), DPP4(1803), ECE1(1889), LAP3(51056)
A4669 Acycloguanosine ≥99% (HPLC), powder Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase.
Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase. Acycloguanosine can be used to induce apoptosis in cells transfected with HSV-TK. Inhibits replication of cytomegalovirus by a mechanism that is independent of its phosphorylation by viral or cellular thymidine kinase.
Antiviral agent.
human ... HV1S(3365), NP(4860)
SML0429 Ac-YVAD-cmk ≥95% (HPLC) Ac-YVAD-cmk is a selective ireversible inhibitor of caspase-1 (interleukin-1β converting enzyme, ICE) with some activity also against caspase-4. Ac-YVAD-cmk is anti-apoptotic and has anti-inflammatory and neuroprotective effects, thought to result from its preventing caspase-1 activation of the proinflammatory cytokine, Interleukin-1β.
SML0928   AD-01 trifluoroacetate salt ≥95% (HPLC) AD-01 is a potent antiangiogenic peptide a FKBPL fragment, which interact with cell-surface receptor CD44. AD-01 inhibits the self-renewal capacity of CD44-positive breast cancer stem cells (BCSC).
SML2300 ADA-07 ≥95% (HPLC) ADA-07 is a potent and selective T-LAK cell-originated protein kinase (TOPK) inhibitor that binds to ATP-binding pocket. ADA-07 suppresses SUV-induced phosphorylation of ERK1/2, p38, and JNKs and subsequently inhibited AP-1 activity, and reduces SUV-induced skin carcinogenesis.
A7486 Adapalene ≥98% (HPLC) Adapalene is a synthetic derivative of naphthoic acid. It possesses retinoid activity. Adapalene is involved in regulating cellular keratinization and inflammatory process.
Adapalene, also referred as Differin, is a derivative of naphthoic acid. It is widely used for topical treatment of acne vulgaris. Adapalene elicits anti-inflammatory and retinoid-like activity. It also has a potential to regulate keratinization and differentiation of follicular epithelial cells.
Retinoic acid analogue that is a RARβ and RARγ agonist (AC50 values are 2.2, 9.3, 22 and > 1000 nM for RARβ, RARγ, RARα and RXRα receptors respectively). Inhibits proliferation and induces apoptosis in colorectal cancer cells in vitro. Displays comedolytic activity. Its unique pharmacological properties make it superior to other retinoids for the treatment of acne.
SML1110 Adaphostin ≥98% (HPLC) Adaphostin is a p210bcr/abl tyrosine kinase inhibitor displaying anti-proliferative activity in leukemia models, human prostate cancer cell line PC-3 and other cancer cell lines. Adaphostin is a potent inducer of myeloid cell death. Similarly to AG957, adaphostin appears to induce a degradation of WT and mutated Bcr/Abl.
SML1940 ADDA 5 hydrochloride ≥98% (HPLC) ADDA 5 is a potent and selective inhibitor of cytochrome c oxidase (Complex IV) that depletes the bioenergetics reserve capacity in intact glioma cells. ADDA 5 specifically inhibits the proliferation of chemosensitive and chemoresistant glioma cells, while sparing non-cancer cells. Additionally ADDA 5 is effective against glioma stem cells.
SML0240 Adefovir ≥98% (HPLC) Adefovir is an antiviral drug that after intracellular conversion to adefovir diphosphate inhibits hepatitis B virus (HBV) DNA polymerase (reverse transcriptase).
Adefovir, also known as 9-(2-phosphonylmethoxyethyl)adenine (PMEA), is an acyclic nucleoside phosphonate. It has a potential to hinder the in vitro replication of several retroviruses such as human immunodeficiency virus (HIV)-1 and HIV-2, simian immunodeficiency virus (SIV), simian AIDS-related virus (SRV), feline immunodeficiency virus (FIV). Thus, Adefovir may be used as a therapeutic for various retrovirus infections including acquired immunodeficiency syndrome (AIDS).
A9251 Adenosine ≥99% Endogenous neurotransmitter at adenosine receptors. Cardioprotective effects may relate to activation of A1 adenosine receptors. The antiplatelet and anti−inflammatory actions of adenosine appear to be mediated via the A2 adenosine receptor. In contrast, adenosine appears to be a pro-inflammatory mediator in asthma and chronic obstructive pulmonary disease (COPD).
human ... ADA(100), ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140), ERBB2(2064), ERBB4(2066)
rat ... Adcy2(81636), Adora1(29290), Adora2a(25369), Adora3(25370)
01890 Adenosine Endogenous neurotransmitter at adenosine receptors. Cardioprotective effects may relate to activation of A1 adenosine receptors. The antiplatelet and anti−inflammatory actions of adenosine appear to be mediated via the A2 adenosine receptor. In contrast, adenosine appears to be a pro-inflammatory mediator in asthma and chronic obstructive pulmonary disease (COPD).
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
A111 Adenosine amine congener hydrate solid, ≥98% (HPLC) Potent aqueous-soluble A1 adenosine receptor agonist.
rat ... Adora1(29290)
A5285 Adenosine 5′-diphosphate monopotassium salt dihydrate bacterial, ≥95%, powder P2Y receptor agonist.
human ... HSP90AA1(3320), P2RY1(5028)
A9501 Adenosine 3′,5′-cyclic monophosphate ≥98.5% (HPLC), powder Naturally-occurring activator of cyclic-AMP-dependent protein kinase (PKA). cAMP is an important second messenger that is linked in many systems to neurotransmitter- or hormone-induced receptor stimulation. The cAMP/PKA signaling pathway has been shown to inhibit cell proliferation, induce differentiation and lead to apoptosis.
human ... OPRK1(4986)
A6885 Adenosine 3′,5′-cyclic monophosphate sodium salt monohydrate ≥98.0% (HPLC), powder Naturally-occurring activator of cyclic-AMP-dependent protein kinase (PKA). cAMP is an important second messenger that is linked in many systems to neurotransmitter- or hormone-induced receptor stimulation. The cAMP/PKA signaling pathway has been shown to inhibit cell proliferation, induce differentiation and lead to apoptosis.
A2224 Adenosine 3′,5′-cyclic monophosphate acetoxymethyl ester >97% (HPLC) Membrane-permeable precursor of the second messenger cyclic AMP
A166 Sp-Adenosine 3′,5′-cyclic monophosphorothioate triethylammonium salt hydrate ≥98% (HPLC), solid Sp-Diastereomer of adenosine 3′,5′-cyclic monophosphorothioate is a potent, membrane-permeable activator of cAMP dependent protein kinase I and II that mimics the effects of cAMP as a second messenger in numerous systems while being resistant to cyclic nucleotide phosphodiesterases; exhibits greater specificity and affinity than forskolin and cAMP analogs such as dibutyryl-cAMP.
A165 Rp-Adenosine 3′,5′-cyclic monophosphorothioate triethylammonium salt powder, ≥98% (HPLC) Rp-Adenosine 3′,5′-cyclic monophosphorothioate triethylammonium salt is capable of inhibiting protein kinase A (PKA).
Rp-Diastereomer of adenosine-3′,5′-cyclic monophosphothioate. Specific membrane-permeable inhibitor of activation by cAMP of cAMP-dependent protein kinase I and II; resistant toward cyclic nucleotide phosphodiesterases; blocks cAMP-mediated effects in numerous systems.
A8016 Adenosine 5′-[β-thio]diphosphate trilithium salt ≥80% (HPLC) P2Y receptor agonist.
SML0998   AdipoRon ≥98% (HPLC) AdipoRon is an adiponectin agonist that binds to and activates adiponectin receptors AdipoR1 and AdipoR2, activating AMPK and PPAR-α pathways, and ameliorating insulin resistance and glucose intolerance in mice fed a high-fat diet in a manner similar to adiponectin itself. AdipoRon did not affect body weight, but did increase the expression of genes involved in fatty-acid oxidation, decreased tissue triglyceride content, and prolonged the shortened lifespan of db/db mice.
Oral administration of adipoRon reduced postischemic oxidative stress showing lower expression of NADPH (Nicotinamide adenine diphosphate) oxidase and superoxide production in mouse model. Hence, adipoRon might be considered as a cardioprotective molecule.
SML2271 ADX-47273 ≥98% (HPLC) ADX-47273 is a brain-penetrating, potent and selective metabotropic glutamate receptor 5 (mGlu5; mGluR5) positive allosteric modulator (PAM) that enhances glutamate-stimulated Ca2+ response in rat cortical astrocytes (EC50 = 170 nM, Emax = 380%; [glutamate] = EC20 = 200 nM) via direct mGlu5 binding in a MPEP-, but not Quisqualate-, competitive manner (Ki = 4.3 μM against 2 nM MPEP; rat mGlu5 HEK293) with little mGlu5 agonist activity, no potency toward other rat/human family III GPCRs (mGlu1–8 and GABA-B), nor affinity to 56 GPCRs/transporters/enzymes/ion channels. ADX-47273 shows in vivo antipsychotic-like and procognitive efficacy in mice and rats in vivo (1-300 mg/kg i.p.) with good pharmacokinetic properties (B/P ratio >2, bioavailability ∼40%, T1/2 ∼2 hrs in rats).
SML1829 ADX71743 ≥98% (HPLC) ADX71743 is a brain-penetrant, selective and potent negative allosteric modulator of metabotropic glutamate receptor 7 (mGlu7). In one study ADX71743 exhibited an anxiolytic-like profile in rat and mouse models without causing impairment of locomotor activity. In another study it induced absence epileptic seizures and lethargy.
ADX71743 is known to negatively regulate the effect of mGlu7 (metabotropic glutamate receptor subtype 7), which is associated with a number of anxiety disorders.
SML0457 AE9C90CB ≥98% (HPLC) AE9C90CB is a muscarinic acetylcholine receptor antagonist with 20-fold selectivity for M3 receptor subtypes compared to M2. In an in vivo assay, AE9C90CB was approximately 5 times more selective for inhibiting carbachol-induced urinary bladder contraction, compared to saliva production.
SML1400 AEE788 ≥98% (HPLC) AEE788 is an orally available and potent dual family of human EGFR and VEGFR receptor tyrosine kinase inhibitor that exhibits potent antitumor and antiangiogenic activity.
human ... EGFR(1956), ERBB2(2064), FLT1(2321), KDR(3791)
SML0264 AEG 3482 ≥98% (HPLC) AEG3284 is a compound that binds to HSP90, leading to heat shock factor 1 (HSF1) dependent expression of HSP70, an endogenous inhibitor of JNK activity. Treatment of PC12 cells with AEF3284 blocks JNK dependent apoptosis.
SML1556   AEM1 ≥98% (HPLC) AEM1 (ARE expression modulator 1) is also a selective inhibitor of sirtuin 2, which is a protein deacetylase mediated by NAD+. Sirtuin 2 supports tumor cell proliferation, thus its inhibition stimulates cell death in tumors.
AEM1 is a potent inhibitor of deregulated Nrf2 transcriptional activity. AEM1 broadly decreases the expression of NRF2 controlled genes and sensitizes A549 cells to various chemotherapeutic agents.
SML0706   2-AEMP trifluoroacetate salt ≥97% (NMR) 2-AEMP is a competitive GABAC antagonist with a rapid onset of, and release from inhibition.
SML2737 AER-271 ≥98% (HPLC) AER-271 is a phosphonate precursor (prodrug) form of the selective aquaporin 4 (AQP4) inhibitor IMD-0354 (AER-270; hu/m/r IC50 = 420/390/210 nM using respective CHO AQP4 transfectants) with >5000-fold enhanced solubility. AER-271 is rapidly converted to AER-270 in vivo (plasma AER-270 Cmax = 500 ng/mL or 1.75 μM, 20 min post 10 mg AER-271/kg i.p.; C57BL/6 mice) and exhibits therapeutic efficacy in rodent models of brain damage by cardiac arrest or ischemic stroke (5-10 mg/kg ip. & 0.08 mg/h sc. in mice; 1-10 mg/kg iv. in rats).
SML0435 AF-DX 116 ≥98% (HPLC) AF-DX 116 is a selective M2 muscarinic acetylcholine receptor antagonist.
SML0620   AF-DX 384 Free Base ≥98% (HPLC) AF-DX 384 Free Base is a potent muscarinic M2/M4 receptor selective antagonist (pKi values are 8.22, 8.00, 7.51, 7.18 and 6.27 at human M2, M4, M1, M3 and M5 receptors respectively).
A6636 Aflatoxin B1 from Aspergillus flavus from Aspergillus flavus Green Alternative Aflatoxin B1 is a carcinogenic compound produced by Aspergillus flavus, a common soil fungus, that induces transversion of G to T at codon 249 of the p53 tumor suppressor gene. Aflatoxin B1 is a food contaminant and a hepatocarcinogen. Aflatoxin is biotransformed to genotoxic intermediates by P450 Phase I enzymes, mainly CYP3A4 via aflatoxin B1 3-hydroxylation. Detoxification depends on Phase II enzymes, such as Glutathione S-Transferase and AFB(1)-aldehyde reductase (AFAR). Aflatoxin B1 is a CYP1A2, CYP2A6, CYP2D6, and CYP3A family substrate.
A9887 Aflatoxin B2 Aflatoxin B2 is a hepatocarcinogen. Food contaminant produced by Aspergillus flavus, a common soil fungus. Aflatoxin B2/AFB2 may have dangerous hepatotoxic, teratogenic and carcinogenic actions on various forms of livestock.
A0138 Aflatoxin G1 from Aspergillus flavus Hepatocarcinogen. Food contaminant produced by Aspergillus flavus, a common soil fungus.
A0263 Aflatoxin G2 Hepatocarcinogen. Food contaminant produced by Aspergillus flavus, a common soil fungus.
A6428 Aflatoxin M1 from Aspergillus flavus Aflatoxin M1 possesses hepatocarcinogenic properties.
A6655   Aflatoxin B1−BSA Conjugate from Aspergillus flavus    
A6412   Aflatoxin M1–BSA Conjugate    
A9441   Aflatoxin B + G mixture dry concentrate    
SML1578   Aftin-4 ≥98% (HPLC) Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor. Aftin-4 increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with AD. Aftin-4 can thus be used to induce a rapid, acute Alzheimer′s disease-like toxicity in the rodent brain.
A9486 AG-09/1 ≥98% (HPLC) AG-09/1 is a selective formyl peptide receptor 1 (FPR1) agonist; it activates chemotaxis in human neutrophils. Formyl peptide recetors (FPRs) are GPCRs mainly expressed in phagocytic leukocytes but with lower expression in many other cell types. Formyl peptides, act as Alarmins and are released from bacteria and damaged mitochondria, serving as chemoattractants for phagocyte recruitment to sites of inflammation, resulting in immune response. Because the endogenous ligands for FPRs are peptides and arachadonic acid metabolites, there are few small molecule tools for these receptors. A recent HTS of commercially available libraries yielded several FPR-1 selective agonists, of which AG-091 was the most potent. AG-091 induced intracellular calcium flux in FPR-1- but not FPR-2-expressing cells. It also caused chemotaxis and intracellular calcium flux in human leukocytes. AG-091 is a valuable tool for studying FPR1 function in immune and other disease states.
PZ0268 AG-17724 ≥98% (HPLC) AG-17724 is a potent peptidyl-prolyl isomerase (PPIase) Pin1 inhibitor.
A1487 AG-205 ≥98% (HPLC) AG-205 is a Pgrmc1 (progesterone receptor membrane component 1) inhibitor. AG-205 alters the spectroscopic properties of the Pgrmc1-heme complex. AG-205 inhibits cancer cell viability and cancer cell progression. acting preferentially on Pgrmc1-expressing cells.
Pgrmc1 is a cytochrome associated protein. It is found to be upregulated in several cancer types such as breast, lung and gastric cancer. Pgrmc1 regulates the epidermal growth factor signaling.
SML0895   AGI-6780 ≥98% (HPLC) AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.
A9219   Agitoxin-2 from scorpion venom recombinant, expressed in E. coli, ≥98% (SDS-PAGE), lyophilized powder Potent Shaker K+ channel blocker . Useful as a probe for Kv channels.
A8231 AGK2 ≥97% (HPLC), powder AGK2 is a SIRT2 inhibitor. AGK2 rescues dopamine neurons from α-synuclein toxicity in Parkinson′s disease models. IC50 for SIRT2 = 3.5 uM. AGK2 is >15-fold more selective for SIRT2 than SIRT1 and SIRT3. AGK2 may be the most selective SIRT2 inhibitor available.
SML2034 AGN 193109 ≥98% (HPLC) AGN 193109 is an orally active retinoic acid receptor (RAR) antagonist that targets all three RAR subtypes with higher affinity (RARα/β/γ Kd = 2 nM) than all-trans retinoic acid/ATRA (RARα/β/γ Kd = 9/12/19 nM). AGN 193109 potently antagonizes against ATRA-induced transcription in RARα, RARβ, and RARγ transfected CV-1 cells (by 85%, 62%, and 100%, respectively, by equal molar AGN 193109 against ATRA). AGN 193109 is also widely employeed to block RAR-mediated physiological and pathalogical processes in mice and rats in vivo via oral (1-10 mg/kg) or topical (0.3-36 μmol/kg) administration.
SML2665 AGN194310 ≥98% (HPLC) AGN194310 (IRX4310; VTP 194310) is a retinoic acid receptor (RAR) antagonist that targets all three RAR subtypes with higher affinity (RARα/β/γ Kd = 3/2/5 nM) than all-trans retinoic acid/ATRA (RARα/β/γ Kd = 15/13/18 nM) without affecting RXR subtypes. AGN194310 effectively blocks RAR agonist TTNPB-induced transcription activity (using RARα, RARβ, or RARγ transfected cells) and prevents TTNPB toxicity in guinea pigs in vivo (by 79/84/94% at AGN194310/TTNPB ratios of 0.5/2/8). AGN194310 potentiates differentiation in osteoblast cultures (1 μM) and daily oral administration (0.5 mg/kg/d for a10-d period) is reported to cause impaired radial bone growth among 8-wk-old mice.
A1362 Agomelatine ≥98% (HPLC) Agomelatine is an extremely potent agonist at both melatonin receptors (MT1 and MT2), with additional antagonism at 5HT2C. It is a novel antidepressant with many desired in vivo properties, including neuroprotection and neurogenesis in depression-sensitive brain areas. Agomelatine′s efficacy appears to be due to both melatonergic and serotonergic properties. In neurogenesis assays, both in vitro and in vivo, the compound effects were differentially affected by antagonists for MT1/MT2 and 5HT2C, demonstrating actions through all three receptors.
Agomelatine modulates the sleep-wake cycle through its chronobiotic activity. It normalizes the sleep pattern in patients suffering from depression and seasonal mood disorder.
human ... HTR2C(3358), MTNR1A(4543), MTNR1B(4544)
A3477 AH 11110 >98% (HPLC), solid α1B-adrenoceptor ligand
A8227 AH23848 hemicalcium salt ≥90% (HPLC), powder AH23848 regulates nitric oxide (NO) production and reduces endogenous cAMP accumulation. This is carried out by declination of inducible nitric oxide synthase (iNOS) gene expression and acceleration of iNOS protein degradation in glomerular mesangial cells.
EP4 prostanoid receptor antagonist with TP blocking activity.
A1221 AH6809 ≥98%, crystalline solid or supercooled liquid AH6809 plays a role in antagonizing the proliferation of non-small cell lung cancer cell lines.
DP/EP prostanoid receptor antagonist; has the highest affinity for DP receptors, but also acts as a weak antagonist at murine EP1 and EP2 prostanoid receptors.
SML0009 AI-1 ≥98% (HPLC) AI-1 positively regulates antioxidant response element (ARE)-driven gene transcription through the activation of Nuclear factor E2-related factor 2 (Nrf2), an ARE-binding transcription factor.
AI-1 promotes Nrf2 activation via the covalent modification of Kelch-like ECH-associated protein 1 (Keap1), a negative regulator of Nrf2. Biochemical studies indicate that an aromatic chloride present within the AI-1 molecule undergoes a nucleophilic aromatic substitution reaction with cysteine thiols of Keap1.
SML0300 Aib-1 trifluoroacetate salt ≥98% (HPLC) Aib-1 is an inhibitor of β-Amyloid oligomerization. Aib-1 is an endomorphin analog more stable to enzymatic degradation and incorporating the β-breaker 2 aminoisobutyric acid. It interacted with Aβ and markedly inhibited the formation of toxic oligomer and fibril growth using in vitro assays, prevented Aβ toxicity in neuronal PC12 cells, and increased longevity in a fly model of Alzheimer′s disease. Aib-1 activity is thought to be due to multi-mode interactions including aromatic, hydrophobic, and polar contacts with Aβ.
A9978 AICAR ≥98% (HPLC), powder AICAR is a cell permeable activator of AMP-activated protein kinase (AMPK), a metabolic master regulator that is activated in times of reduced energy availability (high cellular AMP:ATP ratios) and serves to inhibit anabolic processes. In vivo, pharmacologic activation of AMPK with AICAR mimics exercise and triggers insulin-independent glucose uptake by skeletal muscle.
SML2143 Ailanthone ≥98% (HPLC) Ailanthone, natural compound isolated from Ailanthus altissima (Simaroubaceae), is a potent inhibitor of androgen receptor (AR) that blocks activities of full-length AR and AR splice variants. It overcomes MDV3100 (Enzalutamide)-resistance in castration-resistant prostate cancer cell lines. Ailanthone disrupts the interaction between AR and the chaperones HSP90, HSP70, and HSP40, which leads to AR ubiquitination and degradation.
A7479 5-AIQ hydrochloride ≥97% (HPLC), solid 5-AIQ hydrochloride is an inhibitor of poly (ADP-ribose) polymerase-1 (PARP-1).
SML1344 AK-1 ≥98% (HPLC) AK-1 is a benzylsulfonamide. It acts as avia inhibiting of the nuclear factor-KB (NF-KB) /CSN2 (casein β) pathway.
AK-1 is a cell permeable, potent and specific SIRT2 inhibitor that induced proteasomal degradation of the Snail transcription factor.
SML0152 AK-7 ≥98% (HPLC) AK-7 is a brain penetrant selective SIRT2 inhibitor. No inhibition of SIRT1 or SIRT3 detected.
In neurons, the sirtuin 2 inhibitor AK-7 is neuroprotective in vitro and decreases polyglutamine inclusions and cholesterol levels. In mice, treatment with brain-permeable SIRT2 inhibitor AK-7 led to improved motor function, extended survival and decreased brain atrophy. AK-7 decreases the polyglutamine aggregation in R6/2 brain.
Selective SIRT2 Inhibitor AK-7 is a brain penetrant selective SIRT2 inhibitor. No inhibition of SIRT1 or SIRT3 detected.
Selective SIRT2 Inhibitor
SML1822 Akebia saponin D ≥98% (HPLC) Akebia saponin D (ASD) is a bioactive triterpenoid saponin isolated from the rhizome of Dipsacus asper Wall that is used as an anti-osteoporosis drug. Akebia saponin D exhibits therapeutic effects in number of disease models including cancer, Alzheimer′s disease, cardiovascular disease, and bone fractures. Akebia saponin D protects against nonalcoholic fatty liver disease (NAFLD) liver damage in mice model of NAFLD. ASD decreases hepatic steatosis and heptocyte apoptosis through autophagy modulation. Akebia saponin D prevents oleic acid induced lipid droplets accumulation and increases autophagic flux BRL cells.
A6730 Akt1/2 kinase inhibitor ≥98% (HPLC) Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.
A3846 AL-8810 ≥98% (HPLC), solid AL-8810 is a novel prostaglandin F analog; selective FP prostanoid receptor antagonist.
human ... PTGFR(5737)
SML1374 Alamandine trifluoroacetate salt ≥98% (HPLC) Alamandine is an endogenous heptapeptide that can be formed from angiotensin A by angiotensin converting enzyme-2 or directly from angiotensin-(1–7) by decarboxylation of its aspartate residue. Alamandine′s activity is similar to Ang-(1–7) rather than that of angiotensin II or angiotensin A. However, Alamandine acts at a different receptor, the Mas-related receptor, MrgD. Alamandine causes vasodilation, and has antifibrosis and antihypertensive activity.
A4665 Alamethicin from Trichoderma viride ≥98% (HPLC) Alamethicin is a monovalent cation ionophore that can mimic nerve action potential across artificial membranes. Alamethicin has also been used to study membrane interactions of antimicrobial peptides.
A5361   Alamethicin, Ready Made Solution from Trichoderma viride 5 mg/mL in DMSO, sterile; 0.2 μm filtered Alamethicin is a 20-amino acid channel-forming peptide antibiotic isolated from the fungus Trichoderma viride. Alamethicin consists of several isoforms, for which structural information has been published. Alamethicin forms voltage-dependent channels across lipid bilayer membranes. The Alamethicin channel is built by a bundle of helical monomers forming a water filled transmembrane pore. The conductivity level of the channel is determined by the number of associated helical monomers (3-12), which generates a non aligned supermolecular structure with an aqueous core through which ions can cross lipid membranes. Alamethicin catalyzes the exchange of protons for monovalent cations with little difference in affinities and has the ability to transport cations through biological and artificial lipid membranes. Alamethicin can be used for the permeabilization of mitochondria without affecting the outer or inner membranes.
SML0415 Alantolactone ≥98% (HPLC) Alantolactone is a sesquiterpene lactone disrupts the Cripto-1/ActRII complexes, resulting in an induction of activin/SMAD3 signaling. Alantolactone inhibits proliferation in cancer cells with no affect on normal cells.
A3227 Ala-Tyr-Pro-Gly-Lys-Phe-NH2 trifluoroacetate salt ≥98% (HPLC), lyophilized powder AYPGK is a ligand for the PAR4 receptor; binding results in activation of PAR4. AYPGK stimulates platelet aggregation in vitro (EC50 =15 μM) via PAR4. In human platelets treated with the PAR4 agonist, AYPGKF stimulates the production of thromboxane, a potent agent for platelet-aggregation. Additionally, AYPGKF mediates the thrombin-induced release of endostatin from rat platelets.
SML1590 Alcaftadine ≥98% (HPLC) Alcaftadine is a potent inverse agonist at H1, H2 and H4 histamine receptors. Alcaftadine is antiallergic agent that exhibit anti-inflammatory and mast cell stabilizing effects.
human ... HRH1(3269)
SML1480   Alclometasone dipropionate ≥98% (HPLC) Alclometasone dipropionate is a glucocorticoid receptor agonist that mimics the metabolic, anti-inflammatory, immunosuppressive, antipruritic, and vasoconstrictive effects of natural glucocorticoids.
SML0462 Alda-1 ≥98% (HPLC) Alda-1 is an ALDH2 agonist; cell-permeable activator of both the wild-type ALDH2*1 and the asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2. ALDH2 is the oxidative enzyme, which removes the ethanol metabolite acetaldehyde and other aliphatic aldehydes. Also. ALDH2 is involved in bioconversion of vasodilator nitroglycerin to nitric oxide. Alda-1 increases acetaldehyde oxidation by ALDH2*1 (wild type) and ALDH2*2 9 Asian variant) approximately 1.5- and 6-fold, respectively. It appears that Alda-1 stimulates acetaldehyde oxidation by ALDH2 by improving NAD binding, but does not improve the nitroglycerin binding affinity of the Asian variant.
SML0317 Aldi-2 ≥95% (HPLC) Aldi-2 is a potent and specific covalent inhibitor of aldehyde dehydrogenases. Apparently, Aldi-2 undergoes an enzyme-mediated β-elimination which generates a vinyl-ketone intermediate that covalently modifies the active site cysteine.
A9477 Aldosterone ≥95% (HPLC) Aldosterone is a biologically active aldosterone isomer; a mineralocorticoid produced by the adrenal cortex. It induces urinary excretion of K+ and renal reabsorption of Na+. It is produced from adrenocorticotropic hormone (ACTH) and is essential for maintaining sodium homeostasis in the distal tubules. Aldosterone binds to the mineralocorticoid receptor and may modulate vascular system and induce kidney damage. It contributes to the progression of chronic kidney disease(CKD). Aldosterone is part of the renin-angiotensin-aldosterone system (RAAS).
human ... SERPINA6(866)
rat ... Ar(24208), Nr3c2(25672)
A4978 Alendronate sodium trihydrate ≥97% (NMR), powder Alendronate sodium trihydrate is a bone resorption inhibitor; farnesyl diphosphate synthase inhibitor (IC50 = 460 nM); CD45 protein tyrosine phosphatase inhibitor.
human ... FDPS(2224)
A8986 Alexidine dihydrochloride ≥95% (HPLC) Alexidine dihydrochloride is a potent and selective PTPMT1 (Protein Tyrosine Phosphatase Localized to the Mitochondrion 1) inhibitor. Alexidine increases insulin secretion by isolated rat pancreatic islets.
A0232 Alfuzosin hydrochloride ≥98% (HPLC), solid Alfuzosin hydrochloride is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
SML2077 Aliskiren hemifumarate ≥95% (HPLC) Aliskiren hemifumarate (ALS) has been used to treat hypertension, alone or with other antihypertensive medications. It is suitable for oral administration. ALS regulates baseline systolic and diastolic blood pressure by blocking the catalytic activity of renin system at its rate-limiting step.
Aliskiren is a potent nonpeptide direct renin inhibitor with an IC50 value of 0.6 nM. It has antihypertensive activity, decreasing plasma renin activity and inhibiting the conversion of angiotensinogen to Angiotensin I by binding to the S3 sub-pocket of renin.
SML0381 ALLO-1 ≥98% (HPLC) ALLO-1 is a Smoothened (Smo) antagonist that inhibits both wild-type and mutant Smo, including D473H SMO mutant. ALLO-1 binds to a different domain of Smo than other known Smo ligands.
A8476 17-(Allylamino)-17-demethoxygeldanamycin ≥98% (HPLC), solid Potent inhibitor of heat shock protein 90 (Hsp90). 17-AAG is a less toxic analog than geldanamycin. It induces apoptosis and displays antitumor effects. 17-AAG inhibits the activity of oncogenic proteins such as N-ras, Ki-ras, c-Akt, and p185erB2.
human ... HSP90AA1(3320), HSP90AB1(3326)
SML0337 S-Allyl-L-cysteine ≥98% (HPLC) S-allyl-L-cysteine is a sulfur containing amino acid found in garlic with antioxidant, anti-cancer, antihepatotoxic, neuroprotective and neurotrophic activity. S-allyl-L-cysteine has potent activity in several animal models of ischemic injury and Alzhemer′s disease.
A114 (+)-N-Allylnormetazocine hydrochloride ≥98% (HPLC) Selective σ1 receptor agonist.
human ... OPRS1(10280)
S168 N-Allyl-(±)-SKF-38393 hydrobromide solid, ≥98% (HPLC) N-Allyl-(±)-SKF-38393 hydrobromide is a selective agonist of D1/D5 dopamine receptors. It mimics the physiological action of dopamine and enhances cognition, memory and learning. It decreases the age-related decline in long-term potentiation of mouse hippocampus. SKF-38393 increases the D1-mediated locomotion in rats.
human ... DRD1(1812)
SML1484 Allyphenyline oxalate ≥98% (HPLC) Allyphenyline is a potent α2C-adrenoceptor/serotonin 5-HT1A receptor agonist and α2A-adrenoceptor antagonist that exhibits anxiolytic effect and antidepressant activity. Allyphenyline attenuates opioid and alcohol withdrawal symptoms including hyperlocomotion and anxiety.
SML1210   Almotriptan malate ≥98% (HPLC) Almotriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Almotriptan has low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower. Affinity for 5-HT(7) and 5-HT(1A) receptors was approximately 40 and 60 times lower than that for 5-HT(1B/1D) receptors, respectively.
JN0001 Alniditan dihydrochloride ≥98% (HPLC) Alniditan is a potent and selective serotonin 5-HT1B/5-HT1D receptor agonist that exhibits antimigraine effects.
SML0346 Alosetron hydrochloride ≥98% (HPLC) Alosetron is a potent and highly selective antagonist of serotonin 5-HT3 receptors, nonselective cation channels found predominantly in the enteric nervous system of the gastrointestinal tract. These receptors are involved in the regulation of visceral pain, colonic transit and GI secretions that can contribute to the pathophysiology of irritable bowel syndrome (IBS). Alosetron is used clinically for treatment of women with severe diarrhea-predominant IBS.
human ... HTR3A(3359)
SML2731 alpha-NETA ≥98% (HPLC) Originally identified as a substrate (ChA or choline)-noncompetitive, slowly reversible choline acetyltransferase inhibitor (human ChAT/BuChE/AChE IC50 = 88 nM/33.3 μM/48.6 μM; does not affect mAChRs, AChE, ChE, CrAT, ganglionic or skeletal muscular nAChRs), α-NETA is a fluorescent molecule (Ex 255 & 297 nm; Em 427 nm) also known for its trace amine-associated receptor 5 (TAAR5 EC50 = 150 nM) agonist and chemokine-like receptor-1 antagonist (IC50 = 375 nM; 7 nM chemerin-induced CMKLR1 β-ARR2 recruitment) potencies both in cultures and in animal disease models in vivo (3-20 mg/kg via ip. or sc. in rats & mice).
A1862 Alpidem ≥98% (HPLC), powder Alpidem is a potent antagonist of peripheral benzodiazepine receptor (PBR) that is located on the outer mitochondrial membrane and interacts with the mitochondrial permeability transition (MPT) pore. Alpidem is an anxiolytic drug from the imidazopyridine family. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor.
human ... TSPO(706)
A8800 Alprazolam Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
A4847   Alsterpaullone ≥98% (HPLC), powder Alsterpaullone (ALP) is a cyclin-dependent kinase (CDK) inhibitor. It is considered as a therapeutic agent for group 3 medulloblastomas. Alsterpaullone modulates the progression of cell cycle. It can arrest cell cycle and stimulate the apoptosis of cancer cells by activating caspase-9 through perturbation of mitochondrial membrane potential.
Potent and selective inhibitor of GSK-3β and CDK5/p25; potent inhibitor of CDK1/cyclin B (IC50 = 0.035 μM).
rat ... Gsk3b(84027)
A8106 Altanserin hydrochloride hydrate ≥98% (HPLC), solid Altanserin hydrochloride hydrate is a specific 5-HT2/serotonergic antagonist.
The radioligand of altanserin, [18F]altanserin is useful as a positron emission tomography (PET)-radioligand for the visualization and quantification of serotonin2A (5-HT2A) receptors.
SML2193 Altenusin ≥98% (HPLC) Altenusin, a non-steroidal fungal metabolite, is a potent and selective agonist of Farnesoid X receptor (FXR) that protects mice from high-fat diet induced obesity. Also it decreases blood glucose level, serum insulin level, and reduces lipid droplets accumulation. Altenusin inhibits trypanothione reductase from Trypanosoma cruzi.
A1312 Alternariol from Alternaria sp. ~96% Alternaria mycotoxins are generally associated with undried food grains post-harvest. The disease caused by Alternaria mycotoxin results in a discolored halo in fruits and spotting in leaves. Alternariol (AOH) is cytotoxic and fetotoxic to microbes and mammalian cells. AOH displays inhibitory effect on cell proliferation and has estrogenic functionality.
A3171 Alternariol monomethyl ether from Alternaria alternata (tenuis)    
SML1347 Alvimopan ≥98% (HPLC) Alvimopan is a gastroprokinetic peripheral mu-opioid receptor antagonist. As a drug, Alvimopan is given to patients undergoing bowel surgery to protect the bowel from the effects of opioid medications that are used to treat pain, blocking the undesirable GI side-effects of the opioid agonists without affecting analgesia or causing withdrawal. Alvimopan does not cross the blood-brain barrier, competitively binding to gastrointestinal tract mu-opioid receptors.
human ... OPRM1(4988)
SML0897 ALX 5407 hydrochloride ≥98% (HPLC) ALX-5407 hydrochloride (NFPS hydrochloride) is a selective irreversible inhibitor of the glycine transporter GlyT1 with IC50 values of 3 nM for GlyT1 compared to 100 μM for GlyT2. ALX-5407 hydrochloride showed no activity at the inhibitory glycine receptor or glycine site of the NMDA receptor (IC50 > 100 mM).
A6478 (R,S)-AM1241 ≥98% (HPLC), solid AM1241 acts as an antinociceptive agent in several animal pain models. It has a potential to delay disease progression in amyotrophic lateral sclerosis (ALS) mouse model. Intrathecal, intravenous or intraperitoneal administration of AM1241 reduces hyperalgesia and allodynia in neuropathic rats.
Selective CB2 cannabinoid receptor agonist
A6226 AM251 >98% (HPLC), solid AM251 is a CB1 cannabinoid receptor antagonist.
mouse ... Cnr1(12801), Cnr2(12802)
rat ... Cnr1(25248)
A0980 AM281 ≥98% (HPLC) Potent and selective CB1 cannabinoid receptor antagonist/inverse agonist
rat ... Cnr1(25248)
SML1804 AM4113 ≥98% (HPLC) AM4113 is a Cannabinoid CB-1 neutral antagonist. AM4113 reduced reward and reinstatement of drug-seeking behavior, reducing cue-induced reinstatement in monkeys trained to self-administer cocaine.
A8843 AM580 ≥98% (HPLC)   human ... RARA(5914), RARB(5915)
SML0327 AM630 ≥90% (HPLC) AM630 is a selective CB2 cannabinoid antagonist/inverse agonist (Ki = 31.2 nM) with > 150-fold selectivity over CB1 receptors.
AM630 is an aminoalkylindole and acts as a competitive antagonist of CP 55,940 and WIN 55,212-2. It also behaves as a competitive antagonist of anandamide and (R)-(+)-arachidonyl-1′-hydroxy-2′-propylamide (AM356).
A1987 AM6545 ≥98% (HPLC) AM6545 helps in decreasing the development of albuminuria, inflammation and expression of markers of fibrosis. It also helps in the down-regulation of nephrin and podocin. It has the ability to repress the ingestion of food and food-reinforced behaviour.
AM6545 is a peripheral CB1 cannabinoid receptor antagonist and appetite suppressant.
A1304 β-Amanitin from Amanita phalloides ~90% (HPLC) Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.
A1260 Amantadine hydrochloride Amantadine hydrochloride is effective against influenza viruses both in vivo and in vitro. It is considered as an antagonist of the N-methyl-D-aspartate (NMDA) type glutamate receptor. Amantadine plays an important role in the release of dopamine, preventing dopamine reuptake and blocking microglial activation and neuroinflammation.
Dopamine releaser used to treat Parkinsonism and drug-induced extrapyramidal reactions.
SML2104 Ambrisentan ≥98% (HPLC) Ambrisentan is an endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). It is 200-fold selective for the the ETA receptor subtype with a Ki of 1 nM for ETA and a Ki of 195 nM for ETB.
A5602 AMD3100 octahydrochloride hydrate ≥97% (NMR), solid AMD3100 is a highly specific chemokine receptor CXCR4 antagonist.
SML1433   AMD3465 ≥98% (HPLC) AMD3465 is a highly selective chemokine receptor CXCR4 antagonist with antiviral and anticancer activity. The chemokine receptor CXCR4 is expressed on a wide variety of leukocytes and is the predominant receptor for stromal cell-derived factor-1 (SDF1, CXCL12) in addition to acting as a co-receptor for HIV entry into cells. AMD3465 blocks surface binding of CXCL12 (SDF-1α). AMD3465 is an antagonist of SDF-1 ligand binding (K(i) of 41.7+/-1.2 nM). AMD3465 was found to halt the progression of an agressive childhood blood cancer, T-cell acute lymphoblastic leukemia (T-ALL), within two weeks of starting treatment in an animal model.
AMD3465 is also termed as{N-[1,4,8,11-tetraazacyclotetradecanyl-1,4-phenylenebis(methylene)]-2-(aminomethyl)pyridine}. It controls oncogenic signaling and invasiveness in vitro. It inhibits breast cancer growth and metastasis in vivo. As a chemokine receptor 4 (CXCR4) antagonist, AMD3465 is ten times more efficient than bicyclam AMD3100.
SML2717 AMG517 ≥98% (HPLC) AMG517 is an orally active, highly potent and selective vanilloid receptor-1 (TRPV1; VR1; capsaicin receptor) antagonist that blocks TRPV1-mediated cellular Ca2+ influx (h/r/m IC50/stimulant = 0.76 nM/1.01 nM/1.9 nM/500 nM capsaicin; 0.62 nM/0.5 nM/0.63 nM/acid (pH 5) using respective CHO transfectants; IC50 >20 μM against TRPV2/3/4, TRPA1, and TRPM8-mediated responses; <45% binding at 10 μM to 87 receptors, enzymes, and ion channels) and exhibits antihyperalgesic efficacy in vivo (capsaicin-induced flinch = ED50 = 0.33 mg/kg rats, p.o.; CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg rats, p.o.).
SML0751   AMG-548 dihydrochloride ≥98% (HPLC) AMG-548 is a potent, selective inhbitor of p38α. The Ki values for each p38 isoform are 0.5, 3.6, 2600 and 4100 nM for p38α, p38β, p38γ and p38δ respectively. AMG-548 inhibits LPS-induiced TNFα production in whole blood assay. AMG-548 has also been shown to inhibit Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε.
A2731 AMG 9810 ≥98% (HPLC), powder AMG 9810 is a potent, non-vanilloid, antagonist of the TRPV1 receptor. IC50 = 17 nM.
AMG 9810 is the cinnamide TRPV1 (vanilloid receptor 1) antagonist, that can prevent eye wiping behavior, stimulated by capsaicin and can inverse hyperalgesia in an animal model of inflammatory pain. It possesses antihyperalgesic properties.
SML2457 Amgen16 ≥98% (HPLC) Amgen16 is an NF-κB-inducing kinase (NIK) inhibitor that selectively disrupts noncanonical NF-κB activation in U-2 OS cells (lymphotoxin β receptor LTβR-/TWEAK recetor FN14-mediated p52 nuclear translocation IC50 = 417 nM/2.517 μM) without affecting canonical NF-κB activation (TNF-α-stimulated p65 (RelA) nuclear translocation IC50 >30 μM). Likewise, Amgen16 (1 μM, 30 min pretreatment) selectively inhibits NFKB2 (p100) mRNA production upon noncanonical NF-κB activation (by 84%; 20 ng/mL TWEAK for 4 h), while exhibiting much smaller effect against canonical NF-κB stimulator-induced NFKB2 production (by 36%; 10 ng/mLTNFα for 4 h).
A9232 AMI-1 sodium salt hydrate ≥98% (HPLC) Protein arginine N-methyltransferases (PRMTs) are involved in post-translational modification implicated in protein trafficking, signal transduction, and transcriptional regulation. AMI-1 does not inhibit lysine methyltransferase activity and does not interact with S-adenosylmethionine (AdoMet), unlike most methyltransferase inhibitors which compete for the AdoMet binding site. AMI-1 can modulate nuclear receptor-regulated transcription from estrogen and androgen response elements; and is a HIV-1 reverse transcriptase inhibitor. AMI-1 is a potent antagonist of NADPH-oxidase-derived superoxide production, but acts as a direct antioxidant rather than indirectly through methyltransferase inhibition.
A5922 Amifostine trihydrate ≥97% (TLC), powder Radioprotective agent. Selectively protects normal tissues from the damaging effects of anti-neoplastic radiation therapy. Selectivity is due to preferential uptake by normal tissues and subsequent metabolic activation to 2-(3-aminopropyl)aminoethanethiol.
A7410 Amiloride hydrochloride hydrate ≥98% (HPLC), powder Selective T-type calcium channel blocker and blocker of epithelial sodium channel. Selective inhibitor of urokinase plasminogen activator (uPA).
human ... ABP1(26), ACCN1(40), ACCN2(41), PLAU(5328), SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340), SLC9A1(6548), TNF(7124)
mouse ... Abp1(76507), Accn1(11418), Accn2(11419), Plau(18792), Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278), Slc9a1(20544)
rat ... Abp1(65029), Accn1(25364), Accn2(79123), Plau(25619), Scnn1a(25122), Scnn1b(24767), Scnn1g(24768), Slc9a1(24782)
A9400 7-Aminoactinomycin D ~97% (HPLC), powder    
SML0628   8-Aminoadenosine ≥98% (HPLC) 8-Aminoadenosine, a ribose nucleoside, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine also inhibits transcription and polyadenylation. 8-Aminoadenosine potently inhibits varies breast cancer cell lines proliferation and activates cell death independent of p53. 8-NH2-Ado is highly cytotoxic to other cancer cell lines.
A0788 3-Aminobenzamide ≥99% (TLC) 3-Aminobenzamide enhances cell death, unscheduled DNA synthesis and repair replication by interrupting the rejoining of DNA strand breaks induced by both ionizing radiations and several alkylating agents. It has an ability to inhibit the activity of nuclear enzyme poly (ADP-ribose) synthetase (PARS). 3-Aminobenzamide exhibits protective action against myocardial reperfusion injury and local inflammation.
mouse ... Parp1(11545)
A3940 1-Aminobenzotriazole Green Alternative 1-Aminobenzotriazole (1-ABT) is used as an in vitro tool in drug discovery. It can differentiate the P450 from non-P450 enzyme systems. 1-ABT exhibits inhibitory action by covalent alteration of the heme prosthetic group in the P450 enzyme.
Suicide inhibitor of cytochrome P450 and chloroperoxidase.
human ... CYP1A2(1544)
A138 Aminobenztropine solid High affinity muscarinic ligand that has been used for affinity purification of muscarinic cholinergic receptors.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
T1694 (E)-4-Amino-2-butenoic acid    
A9345   N-(4-Amino-2-chlorophenyl)phthalimide Anticonvulsant
A0779 p-Aminoclonidine hydrochloride solid α2-adrenoceptor agonist.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
A6355 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione hydrochloride powder, ≥98% (HPLC) 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells. Currently, no specific inhibitors of the ERK proteins exist. Preferentially binds to ERK2 with a Kd of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1, but exhibits little effect on ERK1/2 phosphorylation by MEK1/2.