Bioactive Small Molecules

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SML1424 Ac-YVAD-pNA ≥98% (HPLC) Ac-YVAD-pNA is a very selective chromogenic substrate for caspase-1, a key mediator of inflammatory processes formerly known as interleukin (IL)-1-converting enzyme. Ac-YVAD-pNA is used to determine caspase-1 activity. Cleavage of Ac-YVAD-pNA by caspase-1 releases pNA (p-nitroanilide), which can be quantified spectrophotometrically at 405 nm.
A8236 AN-9 ≥95% (HPLC) HDAC Inhibitor tested as an anti-cancer drug; butyric acid pro-drug
SML2812 AN1 ≥98% (HPLC) AN1 is a brain blood barrier penetrant agent that tether LC3 and mHTT and targets mHTT for autophagosome degradation. AN1 significantly lower mHTT in cortices of HD mice, in cells from patients with Huntington’s disease, and neurons derived from induced pluripotent stem cells. AN1 does not lower wtHTT in fibroblasts from healthy human donors. It appears that AN1 interact with the polyQ stretch.
SML0209 ANA-12 ≥98% (HPLC) The neurotrophin brain-derived neurotrophic factor (BDNF) and its receptor tropomyosin-related kinase B (TrkB) have emerged as key mediators in the pathophysiology of several mood disorders, including anxiety and depression. ANA-12 is a TrkB ligand that prevents activation of the receptor by BDNF with a high potency. It binds selectively to TrkB and inhibits processes downstream of TrkB without altering TrkA and TrkC functions. In adult mice model ANA-12 decreases TrkB activity in the brain without affecting neuronal survival. Mice dosed with ANA-12 show reduced anxiety- and depression related behaviors on a variety of tests predictive of anxiolytic and antidepressant properties in humans. ANA-12 may be a valuable tool for studying BDNF/TrkB signaling and may constitute a lead compound for developing the next generation of therapeutic agents for the treatment of mood disorders. There is also N-T19, which is less potent.
A7236 Anacardic acid Anacardic acid is a HAT (Histone Acetyltransferase) inhibitor.
SML0846   Anagrelide hydrochloride ≥98% (HPLC) Anagrelide is a phosphodiesterase inhibitor with antiplatelet activity (IC50 = 36 nM for inhibition of phosphodiesterase-III). Anagrelide inhibits the maturation of megakaryocytes into platelets, reducing both megakaryocyte hyperproliferation and differentiation. As a drug, anagrelide is antithrombocythemic used for the treatment of overproduction of blood platelets.
Anagrelide is a phosphodiesterase inhibitor with antiplatelet activity.
In human and animals, anagrelide has an inhibitory effect on platelet aggregation. Small doses of anagrelide can generate thrombocytopenia. Anagrelide is not advised during pregnancy. It is effectively used in the treatment of essential thrombocytosis.
SML2519 Anamorelin ≥98% (HPLC) Anamorelin is a non-peptidic ghrelin mimetic and growth hormone (GH) secretagogue. It is an orally-active, brain-penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR). Anamorelin has been shown to increases appetite, overall body weight, lean body mass, and muscle strength in clinical studies with cancer patients suffering from cachexia.
A2736 Anastrozole ≥98% (HPLC) Anastrozole, which contains a triazole functional group, reversibly binds to the cytochrome P-450 component of aromatase. Binding interferes with the catalytic properties of aromatase, which results in inhibition of estrogen synthesis.
The aromatase enzyme converts adrenal androgens to estrogen; this enzymatic activity is the primary source of estrogen production in postmenopausal women. One treatment for estrogen receptor-positive breast cancer in postmenopausal women is through inhibition of aromatase. Anastrozole is a nonsteroidal, benzyl-triazole derivative that inhibits aromatase through competitive inhibition and is used to treat estrogen receptor-positive breast cancer. This compound is considered a third-generation, Type II aromatase inhibitor because it is more selective and less effective (if at all) on other steroidal hormones than first and second generation inhibitors.
A8598 Ancitabine hydrochloride Antineoplastic
SML2385 Andrastin A ≥95% (HPLC) Andrastin A is a meroterpenoid protein farnesyltransferase inhibitor with anticancer activity. It has been shown to inhibit the farnesyltransferase activity of the oncogenic Ras proteins and inhibit the efflux of anticancer drugs from multidrug-resistant cancer cells.
Farnesyltransferase inhibitor with anticancer activity; mycotoxin
A7505 1,4-Androstadiene-3,17-dione 1,4-Androstadiene-3,17-dione is a prohormone that converts to an active steroid through the 17bHSD enzyme. 1,4-Androstadiene-3,17-dione is a metabolite of progesterone.
human ... CYP19A1(1588)
A7755 5α-Androstane-3α,17β-diol Dihydroandrosterone is a testosterone metabolite; affects sperm maturation and survival.
rat ... Ar(24208)
A2480 5α-Androstan-3β-ol powder mCAR (constitutive androstane receptor) inverse agonist; testosterone metabolite.
A8380 5α-Androstan-17β-ol-3-one ≥97.5% Androstanolone is an anabolic steroid. Testosterone secreted by the testis is converted to dihydrotestosterone in the target tissues where it appears to mediate many of the biological actions of testosterone. Androgens direct the development of the male phenotype during embryogenesis and at puberty.
human ... AR(367), ESR1(2099), PGR(5241), SERPINA6(866), SHBG(6462)
mouse ... Esr1(13982)
rat ... Ar(24208), Esr1(24890), Nr3c1(24413), Nr3c2(25672), Pgr(25154)
A7883 5α-Androst-16-en-3α-ol 5alpha-androst-16-en-3alpha-ol (androstenol), is an androgen believed to act as a pheromone.
A3009 4-Androsten-11β-ol-3,17-dione 11β-Hydroxy-4-androstene-3,17-dione is a naturally occurring steroid that is primarily, if not strictly, produced in adrenal tissue. In diseases such as Cushing′s syndrome, adrenal-originated hyperandrogenism, and congenital adrenal hyperplasia, plasma 11β levels are very high. Plasma 11β concentration is very low in congenital 11-hydroxylase deficiency and adrenal insufficiency.
A8008 5α-Androst-16-en-3-one    
E3375 trans-Androsterone   human ... HSD17B3(3293)
SML1373 Angiotensin A trifluoroacetate salt ≥98% (HPLC) Angiotensin A (Ang A) is an endogenous vasoconstrictor octapeptide. It is a derivative of angiotensin II (Ang II) that differs from Ang II in having alanine instead of aspartic acid as the first amino acid. Angiotensin A has similar affinity as Angiotensin II for AT1 and AT2 receptors with Ki values of 1.6 and 2.3 nM at AT1 and AT2 receptors.
A0773 Angiotensin Converting Enzyme Inhibitor ≥95% (TLC)    
10385 Angiotensin III trifluoroacetate salt hydrate ≥98% (HPCE) Angiotensin III is an AT1 and AT2 agonist, with higher sensitivity for the AT2 receptor. Ang III has been shown to be a main effector peptide in RAS-controlled vasopresin release and a stimulator for aldosterone release.
A0230 Angiotensin IV trifluoroacetate salt ≥95% (HPLC), powder AT4 angiotensin receptor agonist. The AT4 receptor appears to be important in synaptic plasticity and thus in learning and memory.
SML2290 ANI-7 ≥98% (HPLC) ANI-7 is a potent and selective activator of the aryl hydrocarbon receptor (AHR) pathway that exhibit potent cytotoxic activity against multiple cancer cell lines while spearing normal breast cells (MCF-10A). Apparently activation of AHR by ANI-7 leads to induction of CYP1 metabolising monooxygenases. ANI-7 metabolites induce DNA damage, checkpoint activation, S-phase cell cycle arrest and cell death in sensitive breast cancer cell lines.
SML1813 Ani9 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), the most potent inhibitor, is the structural analog of Ani7. It may be considered as a novel candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
Ani9 is a potent and highly selective anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A) inhibitor that completely inhibited ANO1 chloride current with submicromolar potency. Ani9 does not affect the intracellular calcium signaling and CFTR chloride channel activity.
SML2288 Anidulafungin ≥97% (HPLC) Anidulafungin is a semisynthetic echinocandin antifungal. Anidulafungin works by inhibiting the enzyme β(1,3)-D-Glucan synthase and thereby disturbing the integrity of the fungal cell wall. This enzyme does not exist in mammalian systems.
A6563 6-Anilinoquinoline-5,8-quinone ≥95% (TLC), solid Blocks cGMP production; inhibits intracellular Ca2+ release; blocks the effects of nitric oxide. Inhibits antigen-induced leukotriene release.
SML0252 Anisodamine ≥98% (HPLC) Anisodamine is a muscarinic receptor antagonist. Anisodamine is a naturally occurring atropine derivative isolated from Scopolia Tangutica Maxim plant indigenous to Tibet.
Anisodamine is a non‐specific cholinergic antagonist. It is considered less efficient and less toxic than atropine. Anisodamine interferes with liposome structure and affects cell membrane. It might act as an anti‐oxidant, in protecting against the damage caused by free radicals. Anisodamine is known to reduce cardiac conduction and also prevents arrhythmia. It can block thromboxane synthesis and might possess anti‐thrombotic function. Anisodamine has been useful in a number therapies including septic shock, circulatory disorders, organophosphorus poisoning, opiate addiction, snake bite and radiation damage. Disorders, such as migraine, gastric ulcers, rheumatoid arthritis, gastrointestinal colic, eclampsia, respiratory diseases, acute glomerular nephritis and obstructive jaundice can be treated with the help of anisodamine.
A9789 Anisomycin from Streptomyces griseolus ≥98% (HPLC), solid Antibiotic isolated from Streptomyces griseolus that inhibits protein synthesis. Acts by inhibiting peptidyl transferase activity in eukaryote ribosomes. Reported to induce apoptosis in a variety of cells including promyelocytic leukemia cells, Jurkat cells, ventricular myocytes, and colon adenocarcinoma cells. Initiates intracellular signals and immediate early gene induction. Selective signaling agonist. Potent Jun-NH2 terminal kinase (JNK) agonist. Activates mitogen-activated protein (MAP) kinases (JNK/SAPK and p38/RK). Antiprotozoal agent.
SML1515 Anle138b ≥98% (HPLC) Anle138b is a fluorescent inhibitor of α-synuclein and prion-protein (PrPSc) aggregation that reduces the progression of prion and Parkinson′s disease in animal models. Anle138b extends the survival of mice infected with prions. Anle138b strongly inhibits BSE-derived and human prions. The fluorescence strongly increases upon binding with α-synuclein fibrils. Apparently, Anie138b binds to hydrophobic pockets in the fibrils.
Anle138b, an oligomer modulator, inhibits neuronal degeneration. It rescues neurons from the aggregation effects of α-synuclein.
SML0728   ANR-94 ≥98% (HPLC) ANR-94 is a potent antagonist of the adenosine A2A receptor (AA2AR). The Ki for human AA2AR is 46 nM. ANR-94 displays neuroprotective properties in rat models of Parkinson′s disease. ANR-94 reverses GABA-A receptor desensitization in oocyte and neuronal electrophysiological preparations.
A8727 Antalarmin hydrochloride ≥98% (HPLC), solid Antalarmin hydrochloride is a non-peptide CRF1 corticotropin-releasing factor receptor antagonist.
Antalarmin serves as a non steroidal inhibitor of pregnancy even during the early stages. It is known to delay parturition. It also prevents the development of gastric ulcers which arises in response to stress.
A9899 Antazoline hydrochloride Imidazoline agonist; more potent than efaroxan in inducing insulin release from β cells; H1 histamine receptor antagonist.
human ... HRH1(3269)
A7475   Anthopleurin-A trifluoroacetate salt >88% (HPLC) Shown to have inotropic effects and not chronotropic effects on mammalian heart preparations.
A8674 Antimycin A from Streptomyces sp. Inhibitor of electron transfer at complex III. Induces apoptosis.
SML0250 anti-3-OS HS peptide trifluoroacetate salt ≥98% (HPLC) MPRRRRIRRRQK is an anti-3-OS HS peptide that binds 3-O sulfated heparan sulfate (3-OS HS) and prevents HSV-1 infection in vivo and in cell culture. It also prevents entry of other members of herpesviruses family including cytomegalovirus (CMV) and human herpesvirus-8 (HHV-8). MPRRRRIRRRQK exhibits protective effects against HSV-1 infection of the mouse cornea.
SML0568   3-AP ≥98% (HPLC) 3-Aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) is a ribonucleotide reductase inhibitor and iron chelator with anti-tumor activity.
3-aminopyridine carboxaldehyde thiosemicarbazone (3-AP) has a IC50 value of 0.3μM. It exhibits anti-proliferative activity in preclinical models of cancer, such as lung cancer. It also has an ability to increase the cytotoxicity, intracellular uptake and DNA incorporation of gemcitabine in vitro.
A7232 AP-18 ≥98% (HPLC), solid AP-18 is a selective TRPA1 channel blocker. Transient receptor potential A1 (TRPA1) plays a central role for chemical sensing in the pain pathway. AP-18 is a novel TRPA1 channel blocker. It reduces cinnamaldehyde-induced nociception in vivo and blocks cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation demonstrating selectivity vs. TRPV11. AP-18 reverses CFA-induced mechanical hyperalgesia in mice.
SML2838 AP20187 ≥98% (HPLC) AP20187 is a synthetic and cell-permeable FK506 (tacrolimus) analog that acts as a chemical dimerizer, a chemical inducer of dimerization (CID), to reversibly dimerize and activate fusion proteins containing a growth factor receptor signaling DmrB domain. It has been used to induce oligomerization of cell surface receptor proteins and to study the activity and/or re-localization of any protein that affected by oligomerization. AP20187 has been found to act as a senolytic. In a transgenic mouse model that expresses the FK506-binding protein–caspase 8 (FKBP–Casp8) fusion protein, AP20187 activated FKBP-fused Casp8 in senescent cells resulting in apoptosis of the cells resulting in delayed tumorigenesis , diminished age-related organ deterioration, and extended life span.
SML2389 AP39 ≥95% (HPLC) AP39 is a anethole dithiolethione (ADT-OH)-derivatized hydrogen sulfide (H2S) donor with a lipophilic & positively charged triphenylphosphonium (TP) moiety for mitochondrially targeted H2S release. AP39 stimulates mitochondrial electron transport and cellular bioenergetic function, protecting against mitochondrial DNA damage and cell death upon oxidative stress induction (effective conc. 30–100 nM; bEnd.3 cells). AP39 in vivo efficacy (0.1-1 μmol/kg i.v.; 0.1-0.3 mg/kg i.p.) is demonstrated in varous rodent models, including neurological damage post cardiac arrest, renal injury post ischemia-reperfusion, burn-caused organ damage, as well as brain atrophy in APP/PS1 mice.
SML2490 APC366 trifluoroacetate ≥97% (HPLC) APC366 is a selective inhibitor of mast cell tryptase, which is involved with allergenic response. It thereby also inhibits protease-activated receptor PAR2, a G-protein-coupled receptor that is activated by mast cell tryptase. Tryptase has been proposed to be involved in fibrosis, joint inflammation and also in promoting breast cancer angiogenesis, all of which APC366 inhibited.
SML2552 AP-C5 ≥98% (HPLC) AP-C5 is a potent and selective inhibitor of the guanosine 3’,5’-cyclicmonophosphate (cGMP)-dependent protein kinase II (cGKII)that selectively blocks cGKII dependent phosphorylation of the vasodilator-stimulated phosphoprotein (VASP) in intestinal organoids. AP-C5 mitigates secretory response provoked by the GCC-activating Escherichia coli heat-stable toxin (STa) in mouse small intestinal tissue.
SML1503 Apcin ≥98% (HPLC) Apcin is an inhibitor of the anaphase-promoting complex/cyclosome (APC/C), a large multimeric complex that functions as a ubiquitin ligase, initiating the metaphase–anaphase transition and regulating ordered transitions through the cell cycle by controlling the ubiquitin-mediated proteolysis of cell cycle proteins. Apcin prevents substrate recognition and inhibits APC/C-dependent ubiquitylation by binding to the D-box binding site of Cdc20, a coactivator required for full activation of APC/C and substrate recognition. The effectiveness of apcin in blocking mitotic exit was synergistically amplified by co-addition of TAME (tosyl-L-arginine methyl ester) or its cell permeable prodrug proTAME, which block Cdc20 binding to the APC/C at a different site than apcin.
A0781 Aphidicolin from Nigrospora sphaerica ≥98% (HPLC), powder Aphidicolin is an antibiotic, a potent antiviral and antimitotic agent and DNA polymerase inhibitor.
human ... POLA1(5422), POLD1(5424), POLG(5428)
SML1342 API-1 API-1 is a potent and specific Akt/PKB inhibitor. API-1 binds to pleckstrin homology (PH) domain of Akt and blocks Akt membrane translocation. The compound inhibits all three members of the family Akt1/PKBa, Akt2/PKBb and Akt3/PKBg. API-1 does not inhibit the activation of PKC, SGK, PKA, STAT3, Erk-1/2 or JNK.
A8851 Apicidin ≥98% (HPLC), from microbial Apicidin is a potent inhibitor of histone deacetylase (HDAC). It particularlyinhibits histone deacetylase 1 and 3 (HDAC1 and HDAC3). Apicidin exhibits anti-protozoal activity against apicomplexan metabolite produced by parasites. It also possesses anti-proliferative activity against several cancer cell lines. Apicidin shows anti-cancer activity against human acute promyelocytic leukemia cell.
SML1055 3-AP-Me ≥98% (HPLC) 3-AP-Me is a dimethyl derivative of the ribonucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me is a potent inducer of ER stress and the unfolded protein response in cancer cell lines, incuding IRE1, PERK and ATF6 activity. Treatment with 3-AP-Me induces CHOP expression, phosphorylation of eIF2α, up-regulation of ATF4 and Bim, and causes mitochondrial membrane depolarization and apoptosis.
A7785   Apolipoprotein C-I from human plasma ≥95% (SDS-PAGE), lyophilized powder Interferes directly with fatty acid uptake and is the major plasma inhibitor of cholesterol ester transfer protein.
human ... APOC1(341)
A7910   Apolipoprotein C-II from human plasma ≥95% (SDS-PAGE) Activates lipoprotein lipase
human ... APOC2(344)
A4393 R-(−)-Apomorphine hydrochloride hemihydrate calcined, ≥98.5% Nonselective dopamine agonist; causes nausea and emesis.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
SML0907 Apoptolidin A Ready Made Solution 1 mg/mL in DMSO Apoptolidin A is a 20-membered macrolide shown to be selectively cytotoxic against several cancer cell lines and noncytotoxic against normal cells. The molecule was originally produced by Nocardiopsis species, and its target site was identified as mitochondrial F0F1-ATPase.
Apoptolidin induces apoptosis selectively in rat glia cells transformed with the adenovirus oncogene E1A. Several minor apoptolidin congeners were isolated, known as Apoptolidins A-D. All apoptolidins were reported to inhibit growth of H292 cancer cells (lung carcinoma) in the submicromolar range. Recently, a stereo-selective synthesis of the Apoptolidin disaccharide was reported.
B3055   Apoptosis PCR Primers Bad primers    
F8425   Apoptosis PCR Primers FAS primer set    
F8300   Apoptosis PCR Primers Fas-Ligand primers    
SML1543 Apratastat ≥98% (HPLC) Apratastat (TMI-005) is an orally active, potent and selective dual inhibitor of disintegrin metalloenzyme 17 (ADAM17/ TACE) and matrix metalloprotease (MMP).
SML2215 Aprepitant ≥98% (HPLC) Aprepitant is an antiemetic drug. It is a moderate cytochrome P450 3A4 (CYP3A4) inhibitor. It is capable of crossing the blood brain barrier in humans. In animals, aprepitant can cross the placental barrier. Aprepitant is a potent and selective antagonist of human substance P/neurokinin 1 (NK1) receptors used clinically to treat chemotherapy-induced or post-operative nausea and vomiting, and being investigated for other activity including possible treatment for depression and pruritis.
A7606 Aprindine hydrochloride ≥98% (HPLC), solid Aprindine hydrochloride is a class Ib antiarrhythmic and hERG channel blocker. Aprindine shows structure similarities to lidocaine and procainamide and is effective in treatment of patients with ventricular premature depolarizations, ventricular tachycardia, and supraventricular arrhythmias. Aprindine inhibits the activation of bovine brain cyclic 3′:5′-nucleotide phosphodiesterase (EC by calmodulin and inhibits calmodulin-stimulated Ca-ATPase (ATP phosphohydrolase EC activity.
SML1805 APS-2-79 hydrochloride ≥98% (HPLC) APS-2-79 is a stabilizer of the Kinase suppressor of Ras (KSR) inactive state, resulting in inhibition of oncogenic Ras signaling, antagonizing the Ras–MAPK pathway. KSR is a MAPK scaffold that is regulated allosterically by dimerization with RAF. APS-2-79 was found to bind to the KSR active site with an IC50 value of 120 nM, antagonizing MEK (MAPKK) phosphorylation by RAF. In Ras mutant cell lines, APS-2-79 increased the potency of several MEK inhibitors..
SML1887 APX2009 ≥98% (HPLC) APX2009 is a cell penetrant potent and selective second-generation inhibitor of APE1 redox-signaling that stimulates APE1 DNA repair activity. APX2009 is neuroprotective against cisplatin and oxaliplatin induced toxicity. APX2009 exhibits potent antitumor activity in neuroblastoma cell lines and 3D spheroid pancreatic tumor model.
SML2381 APY29 ≥97% (HPLC) APY29 has the ability to enhance inositol requiring kinase enzyme 1 α (IRE1α) (P830L)′s oligomeric state to rescue RNase activity.
APY29 is a small molecule that inhibits the kinase activity of IRE1α (in vitro autophosphorylation IC50 = 280 nM) by targeting its active site ATP-binding pocket, while simultaneously acting as an allosteric activator of IRE1α RNase activity (EC50 = 460 nM) by keeping the active site in an open conformation. When applied 1 hr prior to stress induction by 4-hr 6 nM thapsigargin treatment, APY29 significantly potentiates stress-induced unfolded protein response (UPR) in rat insulinoma INS-1 cultures (XBP1 mRNA processing induction = 54% without vs. 78% with 1-hr 3 μM APY29 pretreatment).
SML2587 AQ1 trifluoroacetic acid salt ≥98% (HPLC) AQ1, an anthraquinone derivative, is a potent stabilizer of c-KIT G-quadruplexes (G4) that downregulates c-KIT mRNA and protein expression in human and canine cell lines. Also, AQ1 causes inhibition BCL2 gene expression in HGC27 and MCF7 cells. AQ1 inhibits proliferation of in varies human tumor cell lines including HCG27, MCF7 and imatinib resistant HMC1.2 cells.
SML1883 AR231453 ≥98% (HPLC) AR231453 is a 5-nitropyrimidine derivative that acts as a highly potent and selective GRP119 agonist (EC50/GPR119 species = 0.4 nM/monkey, 1.6 nM/dog, 4.7 nM/hamster, 3.5 nM/human, 12 nM/mouse, 4 nM/rat in cell-based assays), exhibiting no off-target activity toward 216 receptors, enzymes, and orphan GPCRs. AR231453 improves glucose tolerance in mice (3 mg/kg i.p. or 20 mg/kg, p.o.) and rats (3 mg/kg i.p.), while no in vivo efficacy is observed among GPR119-deficient mice.
SML1339 AR420626 ≥98% (HPLC) AR420626 is a selective agonist of Free Fatty Acid 3 receptor FFA3 (previously called GPR41). FFA3 is expressed in adipose tissue, gut, and the peripheral nervous system and normally activated by short chain fatty acids (SCFAs) produced in the body through the fermentation of complex carbohydrates by the gut microbiota. There is increasing interest in the role of the various free fatty acid receptors and SCFAs as chemical messengers in energy regulation and regulation of inflammatory processes and as therapeutic targets in the treatment of various metabolic and inflammatory conditions. AR420626 has an EC50 value of 117 nM for FFAR3 and did not activate FFAR2 in concentrations up to 100 μM.
SML0921   AR7 ≥98% (HPLC) AR7 is an atypical retinoic acid receptor α (RARα) antagonist. There is high interest in retinoic acid receptors for cancer and for differentiation studies. Recently, it has been found that signaling through retinoic acid receptor α (RARα) inhibits chaperone-mediated autophagy (CMA). Disruption of RARα signaling has a stimulatory effect on CMA, but can lead to inhibition of macroautophagy. AR7 antagonizes only the CMA inhibitory effect without affecting macroautophagy, allowing the two RARα effects on autophagy to be studied independently.
A4233 Ara-G hydrate ≥98% (HPLC), solid Ara-G is an inducer of apoptosis; inhibitor of DNA synthesis; antineoplastic; and antimetabolite. Ara-G is converted by cellular kinases to the active 5′-triphosphate, Ara-GTP. Incorporation of Ara-GTP into DNA leads to inhibition of DNA synthesis and apoptosis.
A3230 AR-A014418 ≥98% (HPLC), solid Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 μM) or 26 other kinases, demonstrating high specificity for GSK3.
SML1395 Arachidonic acid sodium salt from Mortierella alpina ≥98.5% (GC) Released arachidonic acid (AA) reacts with molecular oxygen nonenzymatically, through oxidative stress, and enzymatically through the action of oxygenase enzymes. AA is oxidized to prostaglandins and thromboxanes by at least two cyclooxygenase (COX) isoforms, to leukotrienes and lipoxins by lipoxygenases, and to epoxyeicosatrienoic acids via cytochrome p450-catalyzed metabolism. Cellular uptake of arachidonic acid is energy dependent and involves protein-facilitated transport across the plasma membrane.
A8848 Arachidonoyl dopamine ≥98% (HPLC), ethanol solution AA-DA competitively inhibits fatty acid amide hydrolase (IC50 = approx. 22 μM) from N18TG2 neuroblastoma cells and inhibits binding (Ki = 0.25 μM) of the selective cannabinoid receptor subtype 1 (CB1) ligand, [3H]SR141716A, to rat brain membrane. AA-DA also inhibits the anandamide membrane transporter in BL-2H3 basophilic leukemia and C6 glioma cells. AA-DA has at least a 40 fold greater selectivity for CB1 than CB2 receptors in rat brain membranes and has been shown to be more potent than anandamide as a CB1 agonist in undifferentiated N18TG2 neuroblastoma cells. AA-DA induces hypothermia and immobility, and decreases spontaneous activity and pain perception in mice and rats, which supports its action as a CB1 agonist in vivo. AA-DA has been shown to inhibit (IC50 = 0.25 μM) proliferation of human breast MCF-7 cancer cells.
A7357 Arachidonoylserotonin ≥98% (HPLC), oil Arachidonoylserotonin is a Fatty Acid Amide Hydrolase (FAAH) Inhibitor and Transient Receptor Potential Vanilloid-Type I (TRPV1) Antagonist. FAAH and TRPV1 are targets for chronic pain treatment. Arachidonylserotonin is a dual target agent and is analgesic in rodents.
A9719 Arachidonyl-2′-chloroethylamide hydrate ≥97% (HPLC), oil Potent and selective neuronal CB1 cannabinoid receptor agonist.
mouse ... Cnr1(12801), Cnr2(12802)
rat ... Cnr1(25248)
A8973 2-Arachidonyl glycerol ~10 mg/mL, ≥98% (HPLC) Endogenous cannabinoid receptor agonist.
human ... FAAH(2166)
rat ... Cnr1(25248), Cnr2(57302)
A231 Arachidonyl trifluoromethyl ketone oil, ≥97% (NMR) Arachidonyl trifluoromethyl ketone (AACOCF3) plays a role in the inhibition of 12-hydroxyeicosatetraenoic acid (12-HETE) and thromboxane B2 produced by the platelets.
Inhibits anandamide hydrolysis in vitro; inhibits phospholipase A2.
human ... PLA2G1B(5319)
SML2352 Aramchol ≥98% (HPLC) Aramchol is a Aramchol is a bile salt fatty acid conjugate (BAFAC) of arachidic acid and cholic acid. It has been shown to reduce liver fat by a dual mechanism of action. It inhibits the activity of liver Stearoyl Coenzyme A Desaturase 1 (SCD1), decreasing the synthesis of fatty acids. In addition, it activates cholesterol efflux by stimulating the adenosine triphosphate–binding cassette transporter A1 (ABCA1). Aramchol has been investigated for treatment for nonalcoholic steatohepatitis, or NASH.
SML0860   Arbidol hydrochloride ≥98% (HPLC) Arbidol hydrochloride (ARB) is a small monocular compound. It is used to prevent severe pneumonia and virus-associated cytokine dysregulation induced by influenza viruses (IFV). ARB also possesses some immunomodulatory properties, including the effects of interferon induction and macrophage activation.
Arbidol is a broad-spectrum antiviral that has demonstrated activity against a number of enveloped and non-enveloped viruses, and is used clinically to treat influenza. Arbidol inhibits viral entry into host cell and stimulates immune response. Arbidol inhibits fusion between the viral capsid and the cell membrane of the target cell, thus preventing viral entry.
A5736 ARC 239 dihydrochloride hydrate ≥98% (HPLC) ARC 239 is a selective α-2B adrenergic blocker. Although ARC-239, like prazosin, also has some alpha-1 antagonist activity, it is used most commomly to differentiate alpha-2A/D from alpha-2B and alpha-2C subtypes rather than for any alpha-1 inhibition..
A0384 Arcaine sulfate salt Potent antagonist at the polyamine site of the NMDA glutamate receptor.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRINA(2907)
SML1667 Arformoterol tartrate ≥98% (HPLC) Arformoterol is the active isomer of formoterol. Arformoterol is a selective β2-adrenergic receptor agonist, a long-acting beta adrenergic agonist (LABA). Arformoterol is a bronchodilator used clinically as an anti-asthmatic and for treatment of chronic obstructive pulmonary disease (COPD).
A4602 Arg-Arg-Ala-pSer-Pro-Val-Ala ≥95% (HPLC) The phosphoseryl peptide RRApSPVA can provide a sensitive evaluation of the majority of acid and alkaline phosphatases, while being refractory to protein phosphatases.
A0487   Argatroban monohydrate ≥98% (HPLC) Argatroban has a high affinity and binds to arginine in thrombin active site resulting in steric hindrance for substrate binding. Argatroban is effective in preventing thrombus formation and favors thrombolysis than unfractionated heparin. It is recommended for acute ischemic stroke treatment.
Argatroban is a potent, seletive, univalent direct inhibitor of thrombin. It directly inhibits thrombin by binding only to its active site (thus univalent) as compared to Bivalent DTIs (hirudin and analogs) which bind both to the active site and exosite 1.
A6757 D-Arginine monohydrochloride ≥98% (TLC)    
SML1570   Arglabin ≥98% (HPLC) Arglabin is a natural product with antitumor and anti-inflammatory activity. Arglabin competitively inhibits the binding of farnesyl diphosphate to farnesyl transferase (FTase), preventing the activation of RAS proto-oncogene by preventing the incorporation of farnesyl pyrophosphate into human H-ras proteins. Arglabin is also an inhibitor of the NLRP3 inflammasome. Arglabin reduces inflammation and plasma lipids and has shown a marked reduction in atherosclerotic lesions.
SML0935   Aripiprazole ≥98% (HPLC) Aripiprazole is a second generation atypical antipsychotic and anti-depressant with partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors. Ki values are 0.34 nM, 0.8 nM, 1.7 nM, and 3.4 nM, respectively, for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors. Aripiprazole is used in the treatment of schizophrenia.
Aripiprazole serves as a ‘dopaminergic stabilizer’. It is used as a potential therapeutic to treat schizophrenia patients. In addition, it is also preferably used to treat attention deficit hyperactivity disorder (ADHD) in patients with Tourette syndrome (TS).
A5512 Aristolochic acid I powder Potent phospholipase A2 inhibitor, including calcium ionophore-induced phospholipase A2 activity in neutrophils. Kidney tumor initiator in experimental animal model.
SML0178 ARL-17477 dihydrochloride hydrate ≥98% (HPLC) ARL-17477 is an nNOS specific inhibitor. The IC50 against rat nNOS is 35 nM and it has 100-fold selectivity over endothelial and inducible isoforms. ARL-17477 penetrates the brain, and reduces infarct size and reduces cerebral blood flow in several different rodent models of ischemic brain injury.
A265 ARL 67156 trisodium salt hydrate ≥98% (HPLC), solid ecto-ATPase inhibitor; prevents metabolism of P2 purinoceptor agonists.
human ... ENTPD2(954)
SML2046 ARM390 ≥98% (HPLC) ARM390 in a δ-selective opioid receptor agonist derivative of SNC80. ARM390 leads to very low levels of receptor internalization, and does not induce acute desensitization of analgesic response compared to SNC80. ARM390 preferentially recruits arrestin 3 to the delta opioid receptor in mice.
SML0039 Armodafinil ≥98% (HPLC) Armodafinil has affinity for dopamine transporters and inhibits the uptake of dopamine in brain areas that are involved in the cognitive performances. It is beneficial for the patients of substance abuse and mental disorders.
Armodafinil is a non-amphetamine, having a half-life of 10−14 hours.
Armodafinil is the R isomer and longer-lasting isomer of racemic modafinil. It is a psychostimulant wake-promoting agent developed for the treatment of narcolepsy, shift work sleep disorder and excessive daytime sleepiness associated with obstructive sleep apnea
human ... SLC6A3(6531)
A8356 ARP 101 ≥98% (HPLC), solid ARP 101 is a MMP-2 selective inhibitor (Gelatinase A, EC; TBE-1; LG4A; MONA; Type IV Collagenase). ARP 101 has diverse physiological roles including wound healing, cancer metastasis, angiogenesis, tissue remodeling in development and embryogenesis. IC50 = 0.81 nM on MMP-2.
SML2049 AR-R17779 Hydrochloride ≥97% (HPLC) AR-R17779 is a nicotinic acetylcholine receptor alpha7 full agonist that targets α7 nAChR with high affinity (Ki = 92 nM/rat α7 against 5 nM α-BTX vs.16 μM/rat α4β2 against 3 nM (-)-nicotine) and selectivity (EC50 = 6.2/10/12.7 μM using human/rat/monkey α7 nAChR-Xenopus oocyte by whole cell voltage clamp, no antagonistic activity against acetylcholine using human α4β2-, α3β4-, α3β2-, α3β2α5-expressing oocytes or antagonistic activity against 5-HT using rat 5HT3a-exxpressing oocytes). AR-R17779 exhibits cognition-improving efficacy in rats (1-20 mg/kg s.c) and mice (1-20 mg/kg i.p.) in vivo and is widely employed for studying other α7 nAChR-dependent physiological functions.
SML2592 Arteether ≥95% (HPLC) Arteether is a semisynthetic artemisinin derivative with antimalarial activity. It has been used for the treatment of chloroquine-resistant Plasmodium falciparum malaria and cerebral malaria, and has also been shown to have anticancer activity.
A9361 Artemether ≥98% (HPLC) Artemether is a methyl ether derivative of artemisinin. It is used against multi-drug resistant strains of the malaria parasite, Plasmodium falciparum, and shows potential in treatment of schistosomiasis.
Artemisinin possesses a highly reactive endoperoxide bridge, which is core for its therapeutic potential. The endoperoxide bond reacts with iron in the erythrocytes with malarial parasite. This leads to the generation of reactive oxygen species (ROS) directly targeting the parasite. Artemisinin also regulates ferroptosis in tumor cells. The α cell transcription factor Arx expression is reduced by artemether. Prolonged exposure of primary islets also resulted in loss if identity in endocrine cell types and their functionality.
SML1093 Articaine hydrochloride ≥98% (HPLC) Articaine hydrochloride helps to alleviate pain and blocks transmission of the pain signal.
Articaine is an amide local anesthetic widely used in dentistry. Articaine acts by inhibition of nerve impulse conduction by blockade of sodium channels.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
SML2923 ARV-771 ≥98% (HPLC) New ARV-771 is a bromodomain and extraterminal (BET) proteins degrader with a HIF-1?-derived von Hippel–Landau (VHL) E3 ligase-binding hydroxyproline and a BET-binding triazolo-diazepine acetamide. ARV-771 induces BET proteins degradation in castrate-resistent prostate cancer (CRPC) cultures (BRD2/3/4 DC50 <5 nM; 22Rv1, VCaP & LnCaP95) and reduces downstream c-Myc transcription with 10-500-fold higher potency than JQ-1, OTX015, and dBET1. ARV-771, but not JQ-1 or OTX015, effectively downregulates CRPC androgen receptor (30-300 nM) and causes CRPC tumor growth retardation/regression in mice in vivo (30 mg/kg s.c.; 22Rv1 and VCaP).
SML0520 Arvanil ≥98% (HPLC), solution (in ethanol) Arvanil is an activator of cannabinoid and vanilloid receptors, and a potent inhibitor of anandamide accumulation. Arvanil inhibits growth of astrocytoma xenograft tumors in mice, mimicing the effect of neural precursor cells, that have been shown to kill TRPV1-expressing tumor cells by secreting endovanilloids.
SML1263 Arylquin 1 ≥98% (HPLC) Arylquin 1 is a potent secretagogue of the tumor suppressor protein prostate apoptosis response-4 (Par-4), selectively inducing apoptosis in a variety of cancer cells. Arylquin 1 acts by binding to vimentin, displacing Par-4 from vimentin for secretion. Arylquin 1 produced a dose-dependent secretion of Par-4 at nanomolar concentrations.
A6486 AS-136A ≥98% (HPLC) AS-136A is a potent measles virus RdRp inhibitor. Measles virus (MV) is a member of the paramyxovirus family. Ribavirin (R9644) is the only drug available for treatment of paramyxoviruses, and it has limited efficacy against MV. A series of small molecules has been developed to inhibit viral RNA-dependent RNA polymerase (RdRp), a protein vital to infection leading to the development of AS-136A, a very potent RdRp inhibitor. AS-136A has high stability and continues to decrease virus titer after 24 hours in physiologic conditions. AS-136A is now used as a positive control in experiments assaying MV inhibition. This compound is a product of the NIH Probes effort, also known as SID 24769845.
SML1906 AS1517499 ≥98% (HPLC) AS1517499 is a potent STAT6 (signal transducer and activator of transcription 6) inhibitor (IC50 = 21 nM against IL-4-dependent reporter activity) that selectively prevents anti-CD3- & IL-4-induced T-helper cell 2 (Th2) differentiation of mouse spleen T cells (IC50 = 2.3 nM), without affecting anti-CD3- & IL-12-induced Th1 differentiation. AS1517499 in vivo effecicacy is demonstrated in various animal models of immunological disorders, including the autoimmune Graves’ disease, antigen-induced bronchial hypercontractility (10 mg/kg i.p.). AS1517499 treatment (10 mg/kg/day i.p.) following early gliomagenesis blockage by a CSF-1R inhibitor is also shown to greatly prolong the survival rate when compared with CSF-1R inhibition alone in a murine model of PDGF-driven glioma (PDG).
AS1517499 moderately inhibits the expression of RhoA (ras homolog family member A). Overexpression of RhoA protein is associated with allergic bronchial asthma.
SML1022   AS1949490 ≥98% (HPLC) AS1949490 is a potent, selective SHIP2 phosphatase inhibitor. AS1949490 activates insulin signaling pathways in liver and lowers glucose levels in diabetic mice.
AS1949490 is also known as (3-[(4-chlorobenzyl)oxy]-N-[(1S)-1-phenylethyl]-2-thiophenecarboxamide). It enhances the phosphorylation of Akt, glucose consumption and glucose uptake in L6 myotubes. AS1949490 has the ability to block gluconeogenesis in FAO (cell line) hepatocytes.
SML1643 AS2444697 ≥98% (HPLC) AS2444697 is a potent and selective inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK-4) that suppresses the progression of chronic renal failure via anti-inflammatory action.
A8981 AS-252424 ≥98% (HPLC), solid AS-252424 is a potent and selective phosphoinositide 3-kinase PI3Kγ inhibitor with IC50 = 30 nM in a mouse model.
A0231 AS 604850 ≥98% (HPLC), solid AS 604850 is a selective PI3Kγ inhibitor
A0233 AS605240 ≥98% (HPLC) AS605240 inhibits human recombinant phosphatidylinositol 3-kinase (PI3K) γ, α, β, and δ by competing with adenosine triphosphate (ATP). It plays a role in protecting injury following ischemic stroke. AS605240 also inhibits the activation of astrocytes under the influence of Interleukin-6 (IL-6) and its soluble receptor (sIL-6R). It reduces collagen deposition and prevents lung inflammation. AS605240 also inhibits the increase of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) expression instigated by bleomycin. It is effective in preventing pulmonary fibrosis by inhibiting the transforming growth factor β1 (TGF-β1) and T lymphocytes infiltration into lungs.
AS605240 is a potent and selective PI3Kγ inhibitor.
SML1692 AS8351 ≥98% (HPLC) AS8351 is an iron chelator that has been found to inhibit of histone demethylase KDM5B (JARID1B), a histone H3K4 demethylase involved in regulation of cell proliferation and stem cell self-renewal and differentiation. AS8351 is thought to inhibit KDM5B by competing with a-ketoglutarate for chelating iron that KDM5B requires as a co-factor.
SML1913 ASB14780 ≥98% (HPLC) ASB14780 is an indole-based selective and potent cytosolic phospholipase A2α inhibitor (IC50 = 20 nM/cPLA2α and >10 μM/sPLA2α). ASB14780 inhibits cPLA2α-dependent inflammatory responses both in cultures and in animals in vivo, including LPS-induced PGE2 production (IC50 = 0.5 μM; mouse peritoneal exudate cells), A23187-induced TXB2 production (IC50 = 0.54 and 0.64 μM using guinea pig and human whole blood, respectively), TPA-induced ear edema (50 mg/kg, p.o.; mice), OVA-induced asthma (5 - 20 mg/kg/d, p.o.; guinea pig), CCl4-induced hepatic fibrosis and high-fat cholesterol diet-induced fatty liver (0.1-0.3 g/kg/d, p.o.; mouse). SB14780 bioavailability is also demonstrated in dog and monkey, albeit at a lower value (F = 34.3%/dog and 30.9%/monkey vs. 89.6%/mouse).
SML0104   Ascochlorin ≥98% (HPLC), from Verticillium hemipterigenum Ascochlorin is a prenyl-phenol compound and a dihydroorotate dehydrogenase (DHODH) inhibitor. It has hypolipidemic functionality and suppresses hypertension as well as immune responses. It is a glycoside, which also elicits inhibition of the respiratory chain cytochrome bc1.
Ascochlorin is an isoprenoid antibiotic produced by Verticillium hemipterigenum, initially identified as an antiviral and antitumor agent. Research also indicates that ascochlorin inhibits the Qi and Qo quinone binding sites of the mitochondria cytochrom bc1 complex. Moreover, ascochlorin activates p53, probably as a result of its inhibitory effect on mitochondrial respiration. In addition, ascochlorin has the ability to suppress the nuclear subscription enzyme protein-1, a nuclear transcription factor activator, which leads to suppression of the extra-cellular enzyme, matrix metalloproteinase-9 (MMP9). The regulation of MMP is implicated in renal development, macrophage differentiation, atherosclerosis, inflammation, rheumatoid arthritis, and tumor invasion. Ascochlorin was also found to be effective against Mx-1, an estrogen lacking breast cancer cell line.
A3835 Ascomycin from Streptomyces hygroscopicus var. ascomyceticus Green Alternative Ascomycin is a strong immunosuppressant. It inhibits allogenic T-lymphocyte proliferation and can bind with high affinity to FKBP and inhibits calcineurin phosphatase in the nM range.
Ascomycin (FK520) possesses high anti-fungal and immunosuppressant activity. Ascomycin has been shown to inhibit the peptidyl-prolyl cis-trans isomerase activity of FK-506-binding proteins of T cells.
A7861 Asenapine maleate ≥98% (HPLC) Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.
G3018   Asialoganglioside GM1 from bovine brain ~98%, lyophilized powder Removing the sialic acid from monosialoganglioside GM1 inhibits its ability to bind cholera toxin. Asialoganglioside GM1 does not block the binding of cholera toxin to cellular GM1.
SML1261 Asimadoline hydrochloride ≥98% (HPLC) Asimadoline is a potent and selective κ-opioid agonist that does not penetrate the blood-brain barrier. Asimadoline produces both analgesic and antidiarrheal effects.
SML1690 ASMI ≥98% (HPLC) ASMI is a cell-permeable, non-toxic, biocompatible, photostable, positively charged, mitochondria targeting styryl-methylpyridinium based compound that acts as a rapid, cysteine selective, sensitive, and ratiometric (F 518 /F 452  nm) fluorescent turn-on probe (0.5 - 40 μM of [Cys]). Under physiological conditions, cysteine thiol reacts with the ASMI acrylate moiety in a time-dependent manner, and induces a facile intramolecular cyclization to release fluorogenic oxystyryl methylpyridinium. ASMI displays high selectivity over other biothiols (Kobs  = 0.75, 0.038, 0.011 & 0.012 min -1  for Cys, Hcy, GSH & Na 2 S, respectively) and with no interference from other biologically relevant amino acids, essential metal ions, and anions, including Na2S. Shown to monitor mitochondrial Cys levels in HeLa cells and in deep tissues (150 μm of penetration depth) by two-photon excited fluorescence microscopy.
11260 L-Aspartic acid hemimagnesium salt dihydrate ≥97.0% (KT)    
A6558 L-Aspartic acid potassium salt ≥98% (HPLC) L-Aspartic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist.
Principal neurotransmitter for fast synaptic excitation.
SML2769 ASS234 ≥98% (HPLC) ASS234 is a brain-penetrant and orally active multi-target small molecule (MTSM) against (acetyl & butyryl) cholinesterases (hAChE/hBuChE IC50 = 0.81/1.82 μM), monoamine oxidases (hMAO-A/B IC50 = 0.27/120 nM), histamine H3 receptor (hH3R Ki = 84.2 nM; hH4R Ki >10 μM) and sigma-1/2 receptors (hS1R/rS2R = 2.82/50.3 nM). ASS234 exhibits antioxidative and neuroprotective effects in SH-SY5Y cultures (5 μM) and demonstrates therapeutic efficacy in neurodegerative disease models in vivo via sc. (0.62 mg/kg/d mice; 5 mg/kg rats), ip. (1 mg/kg mice) or po. (1 & 10 mg/kg mice).
SML2363 AST487 ≥98% (HPLC) AST487 is a N,N′-diphenyl urea, which inhibits growth and calcitonin gene expression in medullary thyroid cancer cells.
AST487 is an orally available type II tyrosine kinase inhibitor (TKI) that exhibits potent antiproliferation activity against FLT3, RET, PDGFR1, but not BRAF, oncogenic fusions/mutations-driven growth (IC50 = 1.8 nM/FLT3-ITD BaF3, 5.1 nM/FLT3 D835I BaF3, 9-27 nM/TEL-PDGFR1 & PTC3-RET BaF3, <1 nM/FLT3-ITD-expressing MV4-11 &amp; MOLM-13) via binding/stablizing target kinases in the inactive “DFG-out” conformation. AST487 effectively suppresses RET- (NIH3T3-RETC634W & human medullary thyroid cancer (MTC) TT cells) and FLT3-ITD-driven (MV4-11) tumor growth in mice in vivo (20-50 mg/kg/day p.o.).
SML0982   Astaxanthin ≥97% (HPLC), from Blakeslea trispora In vivo and in vitro studies propose that astaxanthin (AST) possesses health-promoting activities, signifying its potential use in the prevention of various diseases, such as cancers and Parkinson’s disease. Due to its bright red colour, AST has been used as a food colorant in animal feeds.
Astaxanthin is a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin protects against oxidative stress, inhibiting NF-KB, suppressing pro-inflammatory genes and suppressing production of pro-inflammatory compounds nitric oxide, prostaglandin E2, TNF-α, and interleukin-1β. Astaxanthin′s protection of cells from oxidative stress generated by TNF-α and palmitate has been shown to ameliorate insulin resistance. Astaxanthin has also been shown to be an inhibitor of PPARγ.
A2861 Astemizole ≥98% (HPLC) Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.
human ... HRH1(3269)
SML0856   AT-56 ≥98% (HPLC) AT-56 is a selective orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), one of two synthases involved in the production of Prostaglandin D2 (PGD2) from arachidonic acid. PGD2 is a lipid signaling molecule, which activates two receptors, DP1 involved in centrally mediated processes such as sleep and pain, and DP2 involved and inflammation. The two PGD synthases involved in its synthesis are hematopoietic (H-PDGS) and lipocalin-type (L-PGDS), which acts to form PGD2 in the CNS and other systems but not in inflammatory cells/tissues. AT-56 binds competitively at the enzyme′s catalytic pocket, and has no effect on the production of other PGs or H-PDGS-catalyzed PDG2. AT-56 inhibited PGD2 production by L-PGDS-expressing human TE-671 cells with an IC50 value of 3 μM without affecting production of PGE2 and PGF2, but had no effect on the PGD2 production by H-PGDS-expressing human megakaryocytes.
SML2394 AT9283 ≥98% (HPLC) AT9283 has also been shown to accelerate growth arrest in various xenograft models.
AT9283 is an ATP site-targeting pyrazole-benzimidazole-based molecule with inhibitory potency against multiple kinases, most notably Aurora A/B (IC50 ≤3.0 nM), JAK2/3 (IC50 = 1.2/1.1 nM), Abl T315I (IC50 = 4 nM), GSK3β, FGFR2, VEGFR3 (Flt4), Mer, Ret, Rsk2/3, Tyk2, Yes (IC50 = 1-10 nM). AT9283 also inhibits 72 other kinases/mutations at a reduced potency (IC50 = 10-30 nM against 14, 30-100 nM against 21, 100-300 against 37 targets), while displaying an IC50 >300 nM toward 144 other kinase targets. AT9283 inhibits the growth/survival of multiple solid tumor cell lines in vitro (IC50 = 7.7-20 nM) and shows anti-cancer efficacy in mice via i.p. injection in vivo (67% and 76%HCT116 tumor growth inhibition on day 16, respectively, with 15 and 20 mg/kg b.i.d., two-day on and two-day off; >95% inhibition of Ba/F3 ETV6-JAK2 leukemia proliferation on day 12 with 10 mg/kg b.i.d. on days 2–5 and 8–12).
SML2598 Ataciguat ≥98% (HPLC) Ataciguat (HMR-1766) is a soluble guanylate cyclase (sGC) activator
SML1796 Atazanavir ≥98% (HPLC) Atazanavir is an antiviral HIV protease inhibitor.
SML2308 Atazanavir sulfate ≥95% (HPLC) Atazanavir sulfate is the prodrug of Atazanavir, an antiviral HIV protease inhibitor.
A3355 ATC0175 ≥98% (HPLC), solid ATC0175 is a non-peptide, orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.
Non-peptide, orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.
A7655 Atenolol ≥98% (TLC), powder Selective β1-adrenoceptor antagonist; antihypertensive; antianginal; antiarrhythmic.
human ... ADRB1(153)
rat ... Adrb1(24925)
A143 (S)-(−)-Atenolol powder β1-Adrenergic receptor antagonist; active enantiomer of atenolol.
human ... ADRB1(153)
SML1720   ATI-2341 trifluoroacetate salt ≥95% (HPLC) ATI-2341 is a potent and selective allosteric agonist of chemokine CXC-type receptor 4 (CXCR4) that functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 does not promote β-arrestin recruitment. ATI-2341 promotes the mobilization of PMNs and HSPCs in the peripheral circulation of both mice and monkeys.
A9611 Atipamezole ≥98% (HPLC) Atipamezole elicits affinity towards adrenoreceptor subtypes namely α2A, α2B and α2C. High levels of atipamezole impairs cognitive functions. It also reverses the adrenoreceptor agonist functionalities. Atipamezole shows no affinity towards muscarinic and dopamine or neurotransmitter receptors. Atipamezole when used along with morphine elicits antinociceptive effects.
Atipamezole is a selective α2 adrenergic blocker. Atipamezole is more potent than yohimbine; it is very selective for α2 adrenergic vs α1 sites, but not selelctive for α2 subtypes.
SML2079   ATN-161 ≥98% (HPLC) ATN-161 is a non-RGD based integrin binding peptide derived from the synergy region of fibronectin that inhibits the receptors for integrins alpha-v beta-3 and integrin alpha-5 beta-1. Integrin alpha-5 beta-1 is expressed on endothelial cells and plays a key role in endothelial cell adhesion and migration and may also play a key role in cancer cell invasion and metastasis. ATN-161 was shown to have antiangigenic and antitumor activity.
A3480 Atosiban ≥98% (HPLC) Atosiban efficiently prevent preterm uterine contractions without any major cardiovascular, pulmonary or central nervous system side effects. It has potential to treat preterm labour.
Atosiban is a peptide oxytocin receptor antagonist.
human ... AVPR1A(552), OXTR(5021)
rat ... Oxtr(25342)
A7986 Atovaquone ≥98% (HPLC) Atovaquone is an anti-protozoal mitochondrial electron transport inhibitor; Antimalarial; Antipneumocystic, and has also been used to treat toxoplasmosis. It is an analog of protozoan mitochondrial protein ubiquinone, and acts by inhibiting the cytochrome bc(1) complex via interactions with the Rieske iron-sulfur protein and cytochrome b in the ubiquinol oxidation pocket.
A263 ATPA solid Selective kainate receptor agonist.
human ... GRIK1(2897)
rat ... Gria1(50592), Grik1(29559), Grin2a(24409)
SML2802 ATR-101 ≥98% (HPLC) ATR-101 (PD 132301-02; Nevanimibe HCl) is an orally active, potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT1, SOAT1) inhibtior (IC50 = 52 nM; intestinal microsome from cholesterol-fed rabbits) that reduces plasma cholesterol in both acute (by 77%; 50 mg/kg po.) and chronic (by 80%; 10 mg/kg po.) cholesterol-fed rat models. In addition, ATR-101 is reported to exhibit therapeutic efficacy against adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH), and Cushing′s syndrome (CS).
SML2020 Atrasentan hydrochloride ≥98% (HPLC) Atrasentan is a selective endothelin ETA receptor antagonist with an IC50 of 0.2 nM for ETA compared to 190 nM for ETB receptors. It blocks blocks endothelin induced cell proliferation, and has been investigated as a possible treatment for prostate cancer, and more recently for therapy for diabetic kidney disease.
SML1041   Atreleuton ≥98% (HPLC) Atreleuton is a reversible 5-lipoxygenase inhibitor. Atreleuton exhibits potent and selective inhibition of leukotriene formation both in vitro and in vivo.
A0132 Atropine ≥99% (TLC), powder Atropine is used to treat myopia and ocular axial elongation in Asian children. Small dosage of atropine is used to slow down the heart rate.
Competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133), LOC730413(730413)
mouse ... Chrm1(12669)
rat ... Chrm1(25229), Chrm2(81645), Chrm3(24260), Drd2(24318), Htr1a(24473)
SML2210 AubipyOMe ≥97% (NMR) AubipyOMe is a potent inhibitor of tartrate resistant acid phosphatase (TRAP/ACP5), a metalloenzyme expressed in activated osteoclasts and in macrophages. AubipyOMe exhibited IC50 values of 1.3 μM for TRAP5a and 1.8 μM for TRAP5b and inhibited TRAP activity in murine macrophage and human lung tissue extracts.
SML0177 AUDA ≥98% (HPLC) AUDA is a potent inhibitor of soluble epoxide hydrolase
Inhibition of soluble epoxide hydrolase by AUDA inhibits the metabolism of epoxyeicosatrienoic acids (EETs) and protects end-organs against the damaging effects of salt-sensitive hypertension. AUDA also renders protection against myocardial ischemia-reperfusion injury and cerebral ischemia.
A6733 Auranofin ≥98% (HPLC) Auranofin inhibits various leukocyte activation pathways at multiple sites. Auranofin inhibits the release of inflammatory mediators from human macrophages, basophils, and pulmonary mast cells. The compound also inhibits 5-lipoxygenase in human neutrophils. Auranofin is a disease-modifying antirheumatic drug (DMARD). The compound is a potent inhibitor of selenoenzyme thioredoxin reductase (TrxR), which is involved in defense against oxidative stress. Auranofin is an efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions related to its inhibition of mitochondrial thioredoxin reductase. Auranofin inhibits IKB kinase (IKK) by modifying Cys-179 of the IKKβ subunit 5.
A9861 Auraptene ≥98% (HPLC) Auraptene is an estrogen receptor modulator that also acts as an ACAT inhibitor. It displays anti-tumor effects in several xenograft and chemically-induced murine tumor models. Auraptene induces apoptosis and is anti-proliferative in cancer cell lines. It has agonistic properties against PPARs, and interferes with lipid and cholesterol production by inhibiting ACAT (IC50 = 4 uM).
Auraptene (7-geranyloxycoumarin) possesses anti-oxidant, anti-bacterial, anti-inflammatory and anti-tumor activities.
SML0882   Aurora-A Inhibitor I ≥98% (HPLC) Aurora-A Inhibitor I is a potent inhibitor of Aurora kinase A with an IC50 of 3.4 nM and 1000-fold selectivity for Aurora A over Aurora B (better than VX-680) and even higher for CDKs. Antiproliferative IC50 values were in the vicinity of 1 μM against the human colorectal cancer cell line HCT116.
A0606 Aurothioglucose hydrate ≥96% (titration) Aurothioglucose, a gold compound used clinically to treat rheumatoid arthritis, has recently been found to be a potent PKCiota-Par6 interaction inhibitor, with an IC50 approximately 1 μM. Disruption of this interaction disrupts a rac1 signaling pathway that is required for transformed growth in non-small-cell lung cancer.
SML2632 Autophinib ≥98% (HPLC) Autophinib is an ATP-competitive, potent and selective PI3K type 3 lipid kinase vacuolar protein sorting 34 inhibitor (VPS34 IC50/[ATP] = 19 nM/10 μM & 51 nM/100 μM) that shows significant inhibition against only 45 kinases among a panel of >460 with little or no potency toward mTOR, TBK1 and 12 other phosphatidylinositol kinases (=22% inhibition at 1 μM). Autophinib effectively prevents autophagy induction in MCF7 cells upon amino acid starvation or rapamycin treatment (IC50 = 40 nM and 19 nM, respectively) with similar potency as SAR405 (IC50 = 53 nM and 20 nM, respectively) and VPS34-IN1 (IC50 = 13 nM and 15 nM, respectively). Autophinib enhances MCF7 cell death under starvation condition (EC50 = 264 nM and 234 nM by cytotoxiciy and apoptosis detection, respectively) by preventing autophagy-dependent cell survival.
SML2799 Avanafil ≥98% (HPLC) Avanafil is an orally active, potent and selective phosphodiesterase-5 (PDE5) inhibitor (IC50 = 5.2 nM) with superior PDE5 selectivity (19,000-, >10,000-, 121-fold over PDE1, PDE11, PDE6, respectively) when compared with tadalafil (25-fold over PDE11), sildenafil and vardenafil (375-fold over PDE1 & 16 to 21-fold over PDE6).
PZ0190 Avasimibe ≥98% (HPLC) Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor. It was originally developed as an antilepic drug, and was shown to significantly reduce plasma total triglyceride and VLDL-cholesterol, but later clinical trials were disappointing. ACAT has also been investigated as a potential therapeutic target for Alzheimer′s disease. Recent studies have looked at the effects of avasimibe in reducing amyloid pathology by limiting generation and increasing clearance of diffusible amyloid-beta (Abeta).
PZ0123 Avridine ≥97% (HPLC) Avridine is a potent synthetic adjuvant that can induce arthritis in most rat strains; immunomodulator and interferon-inducing.
PZ0193 Axitinib ≥98% (HPLC) Axitinib (AG-013736) is an orally available, potent (picomolar) and selective tyrosine kinase inhibitor that blocks VEGF receptors 1, 2 and 3. The drug blocks VEGF-mediated endothelial cell survival, tube formation, and downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase.
human ... FLT1(2321), FLT4(2324), KDR(3791)
A7231   AZ11645373 ≥98% (HPLC), solid AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. KB values range from 5-20 nM for human P2X7 receptor inhibition. It is 500-fold less effective ats an inhibitor of rat P2X7 receptor responses.
SML1429 AZ12216052 ≥98% (HPLC) AZ 12216052 is positive allosteric modulator of mGluR8 receptors that reduced measures of anxiety in wild-type male mice.
SML2822 AZ12601011 ≥98% (HPLC) AZ12601011 is an orally active, subtype-selective TGF-β type I receptors active site inhibitor (active-site affinity: ALK4/5/6 Kd = 2.6/2.9/42 nM, ALK1/2/3 Kd = 40/15/40 μM) that prevents ALK4/5/7-mediated Smad2, but not ALK1/2/3/6-mediated Smad1, phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12601011 inhibits 4T1 murine mammary carcinoma growth in cultures (IC50 = 400 nM) and in vivo (50 mg/kg bid. po. mice). AZ12601011 also causes heart valve lesions and physeal dysplasia in rats (150 mg/kg/day po. for 7 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.
SML2819 AZ12799734 ≥98% (HPLC) AZ12799734 is an orally active TGF-β type I receptors active site inhibitor (ALK1/2/3/4/5/6 Kd = 7.1/6.2/40/1/0.74/0.017 μM) that inhibits ALK5-dependent Smad2 nuclear translocation upon TGF-β1 stimulation (IC50 = 17 nM; MDA-MB-468), as well as ALK1/2/3/6-mediated Smad1 and ALK4/5/7-mediated Smad2 phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12799734 oral administration in rats results in heart valve lesions (200 mg/kg/day for 5 days) and physeal dysplasia (400 mg/kg/day for 6 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.
SML2924 AZ1729 ≥98% (HPLC) AZ1729 is a short chain fatty acid receptor FFA2 (GPR43) regulator that acts as a direct allosteric agonist and as a positive allosteric modulator (PAM). AZ1729 selectively enhances Gi-mediated signaling (Gi-biased ligand), but not at those transduced by Gq/G11 pathway.
SML1089 AZ191 ≥98% (HPLC) AZ191 is a cell permeable, potent and selective inhibitor of DYRK1B that promotes a G1 cell cycle arrest.
SML1328 AZ20 ≥98% (HPLC) AZ20 is cell penetrant potent and selective ATR (ataxia telangiectasia and Rad3-related protein) kinase inhibitor that potently inhibits the growth of LoVo colorectal adenocarcinoma xenografts in mice.
SML1427 AZ3146 ≥98% (HPLC) AZ3146 is a potent and specific inhibitor of monopolar spindle 1 kinase (Mps1; IC50 = 35 nM), an important regulator of Spindle Assembly Checkpoint (SAC). AZ3146 treated HeLa cells override SAC, and quickly enter mitosis, with a reduced mitosis completion time of 32 minutes. 50% of treated cells entered anaphase without complete chromosomal alignment.
SML2551 AZ32 ≥98% (HPLC) AZ32 is an orally active, potent and selective ataxia telangiectasia mutated (ATM) kinase inhibitor (IC50 <6.2 nM; DNA-PK & PI3Ka IC50 =4.6 μM, hERG IC50 = 17.6 μM) with good aqueous solubility (24 μM) and blood-brain barrier (BBB) permeability in mice (free brain/plasma ratio = 0.26; 200 mg/kg p.o.). AZ32 exhibits radiosensitizing efficacy in human & murine glioma cultures by blocking radiation-induced DNA damage response (ATM pS1981 IC50 = 310 nM; 100% blockage of KAP1 pS824 & p53 pS15 at 300 nM; T98G cells). AZ32 (200 mg/kg/day p.o.) improves whole-head irradiation treatment survival rate among mice with brain GL261 tumors or NCI-H2228 NSCLC metastases in vivo.
SML2150 AZ6102 ≥98% (HPLC) AZ6102 is a potent and selective Tankyrase 1/2 (TAMKS1/2) inhibitor that has 100-fold selectivity against other PARP family enzymes. AZ6102 is moderately orally bioavailable in rat and mice.
SML0785   AZ628 ≥98% (HPLC) AZ628 is a potent Raf kinase inhibitor with IC50 values of 105 nM for wild-type B-raf, 34 nM for Raf-B V600E and 29 nM for wild-type c-Raf-1. AZ628 is a type II inhibitor that binds to the catalytically inactive Asp-Phe-Gly (DFG)-out configuration.
A2385 5-Azacytidine ≥98% (HPLC) 5-Azacytidine (Aza-CR) acts as a potential chemotherapeutic regimen for acute myelogenous leukemia. This drug has an ability to selectively increase γ-globin synthesis. Therefore, 5-azacytidine is used in treating severe β-thalassemia. Aza-CR acts as a potential bacteriostatic, antitumor and mutagenic agent. In addition, it also exhibits various biological activity such as, immunosuppressive, antimitotic, radioprotective and virostatic effects.
A potent growth inhibitor and cytotoxic agent; inhibits DNA methyltransferase, an important regulatory mechanism of gene expression, gene activation and silencing.
Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes.
human ... DNMT1(1786), DNMT3A(1788), DNMT3B(1789)
A3656 5-Aza-2′-deoxycytidine ≥97% 5′-Azadeoxycytidine causes DNA demethylation or hemi-demethylation. DNA demethylation can regulate gene expression by "opening" the chromatin structure detectable as increased nuclease sensitivity. This remodeling of chromatin structure allows transcription factors to bind to the promoter regions, assembly of the transcription complex, and gene expression. Decitabine is an epigenetic modifier that inhibits DNA methyltransferase activity which results in DNA demethylation (hypomethylation) and gene activation by remodeling "opening" chromatin. Genes are synergistically reactivated when demethylation is combined with histone hyperacetylation.
human ... DNMT1(1786), DNMT3A(1788)
A3734 1-Azakenpaullone ≥97% (HPLC) 1-Azakenpaullone (AZP) can stimulate the transcription of β-catenin-related genes. This compound can induce the multiplication and replication of β cell.
1-Azakenpaullone is a cell permeable, potent, selective inhibitor of glycogen synthase kinase 3β (GSK3β) with 100-fold less cross-reactivity against CDKs. 1-Azakenpaullone can be used together with BIO and CHIR99021 as "gold standards" for GSK3 inhibition.
SML0485 Azamulin ≥98% (HPLC) Azamulin is a derivative of the antibiotic pleuromutilin. The compound is a very specific inhibitor of the CYP3A family (IC50 = 0.03-0.24 μM). Azamulin is 15 and 13 fold more active against CYP3A4 compared to CYP3A5 or CYP3A7, respectively, and is at least 100 fold selective over other CYP isoforms, with the exception of CYP2J2 (approximately 50-fold).
SML2491 Azasetron hydrochloride ≥98% (HPLC) Azasetron (Y-25130) is an orally active, potent and selective 5-HT3 receptor antagonist (binding Ki = 0.33 nM against [3H]granisetron/rat small intestine, 2.9 nM against [3H]quipazine/rat cortex; little or no affinity toward H1,d5-HT1A/2, Dopamine D1/2, α1/α2 adrenoceptor, muscarinic receptors) with in vivo antiemetic efficacy (0.1-0.3 mg/kg i.v. & 0.1-1 mg/kg p.o.; dogs, ferrets). Y-25130 inhibits 5-HT-induced bradycardia in anesthetized rats (ED50 = 820 ng/kg i.v.), while concurrent intrahippocampal infusion (1.0 μg/side) prevents memory function impairment caused by muscarinic acetylcholine receptor antagonist scopolamine (3.2 μg/side), but not NMDA receptor antagonist CPP (32 ng/side).
SML0268 AZD1152-HQPA ≥98% (HPLC) AZD1152-HQPA is the active metabolite of AZD-1152, a potent selective Aurora Kinase B inhibitor. AZD1152 is 50-fold selective for Aurora kinase B over Aurora kinase C and over 1000-fold selective for Aurora kinase B over Aurora Kinase A. (IC50s: aurora-A, 1,369 nmol/L; aurora-B, 0.36 nmol/L; aurora-C, 17.0 nmol/L). It is converted in plasma to the active form AZD1152-HQPA, which has been shown to have antineoplastic activity in a variety of animal models and human cancer cell lines.
SML2595 AZD1208 ≥98% (HPLC) AZD1208 is an orally available, potent ATP-competitive pan-Pim kinase inhibitor (Pim-1/-2/-3 Ki = 0.1/1.92/0.4 nM; Pim-1/-2/-3 IC50 = 0.4/5.0/1.9 nM with [ATP] = Km; Pim-1/-2/-3 IC50 = 2.6/164/17 nM with [ATP] = 5 mM) wtih high target selectivity (by binding assay with a 442-kinase panel). AZD1208 exhibits selective antiproliferation potency against high Pim-1/-2-expressing AML cultures (GI50 in 72 h = 20 nM/MOLM-16, 60 nM/EOL-1, 300 nM/Kasumi-3, 600 nM/KG-1a, 900 nM/MV4-11) and displays in vivo efficacy against MOLM-16 xenograft tumor growth in mice (by 89% or 100%, respectively, with 10 or 30 mg/kg/day p.o.)
SML2080 AZD1283 ≥98% (HPLC) AZD1283 is potent non-nucleotide P2Y12 antagonist with a Kd value of 11 nM. It had good antithrombotic activity, inhibiting ADP-induced platelet aggregation. AZD1283 has been used to study the structure of the human P2Y12 receptor.
SML1505 AZD1480 ≥98% (HPLC) AZD1480 is an orally active, potent and selective inhibitor of Janus kinases JAK1 and JAK 2 with selectivity for JAK2 as evidenced by IC50 values of 1.3 nM for JAK1 and <0.4 nM for JAK2 in enzyme assays. AZD1480 inhibits endogenous as well as IL-6 induced STAT3 activation. AZD1480 reduces myeloid cell-mediated angiogenesis and metastasis. AZD1489 is an effective anticancer agent in bot adult and pediatric human tumors.
SML2272 AZD-2098 ≥98% (HPLC) AZD-2098 is an orally active, potent and selective CCR4 antagonist (pIC50 = 7.8/8.0/8.0/7.6 against CCL22 binding to human/mouse/rat/dog CCR4; inactive toward CXCR1/2 & CCR1/2b/5/7/8 at 10 μM) with little or no activity toward a panel of ∼120 receptors/enzymes. AZD-2098 effectively inhibits chemokine-induced cellular responses in vitro (pIC50 = 7.5 against CCL22-induced calcium influx in hCCR4-expressing CHO cells; pIC50 = 6.3 against CCL17- or CCL22-induced chemotaxis of primary human Th2 cells) and exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats in vivo (Emax = 7.5 μmol/kg p.o.; 1 h before and every 12 h after antigen challenge).
SML1858 AZD2461 ≥98% (HPLC) AZD2461, an olaparib analog, is an orally available, potent and selective PARP1 and PARP2 inhibitor that is a poor substrate for drug transporters. AZD2461 exhibits a high efficacy in olaparib-resistant tumors that overexpress P-glycoprotein.
SML2590 AZD3463 ≥98% (HPLC) AZD3463 is an orally available, potent receptor tyrosine kinase (RTK) inhibtor against anaplastic lymphoma kinase ALK (Ki = 0.75 nM; IC50 = 15-21 nM with 5FAM-Srctide as substrate & 30 μM ATP), insulin-like growth factor (IGF)-1 receptor (IGF1R), ROS1 (c-Ros), and Trk-A (NTRK1). AZD3463 effectively inhibits multiple crizotinib-resistant cancer growth and displays in vivo efficacy against FLT3-ITD-dependent MOLM-13 acute myeloid leukemia (AML) as well as NGP (wt ALK) & SH-SY5Y (ALK-F1174L) neuroblastoma in mice (15 mg/kg ip.).
SML2484 AZD3839 ≥98% (HPLC) AZD3839 is a potent and selective BACE1 inhibitor (Ki = 26.1 nM/BACE1, 372.4 nM/BACE2, >25 μM/Cathepsin D by cell-free TR-FRET; hERG IC50 = 4.8 μM) that effectively suppresses cellular BACE1 activity in neuron cultures (sAPPβ release IC50 = 16.7 nM/SH-SY5Y; Aβ40 release IC50 = 4.8 nM/SH-SY5Y AAP695wt, 32.2 nM/N2A, 24.8 nM/guinea pig cortical neurons, 51 nM/murine cortical neurons) and exhibits in vivo Aβ40-, Aβ42-, sAPPβ-reducing efficacy (80 & 160 μmol/kg mouse, p.o.; 100 & 200 μmol/kg guinea pigs, p.o., 2.5 & 20 μmol/kg cynomolgus monkeys, i.v.) with good pharmacokinetic properties and oral availability.
SML1855   AZD5438 ≥97% (HPLC) AZD5438 is an orally active, potent and reversible inhibitor against cyclin-dependent kinases (IC50 = 6 nM/Cyc E-CDK2, 14 nM/p25-CDK5, 16 nM/Cyc B1-CDK1, 20 nM/Cyc T-CDK9, 21 nM/Cyc D3-CDK6, 45 nM/Cyc A-CDK2, 449 nM/Cyc D1-CDK4, 821 nM/Cyc H-CDK7; [ATP] = Km) and glycogen synthase kinase GSK-3β≤ (IC50 = 17 nM) without significant inhibitory potency toward 30 other kinases (≤75% inhibition at 10 μM). AZD5438 effectively inhibits cellular CDK substrates phosphorylation and displays antiproliferation activity against a broad spectrum of human cancer cultures (IC50 from 0.2 μM/MCF to 1.7 μM/ARH-77) by inducing cell cycle arrest at G2-M, S, and G1. Oral administration (50 mg/kg/12 h or 75 mg/kg/day) is efficacious against human tumor xenograft growth in mice in vivo.
SML2900 AZD5582 ≥98% (HPLC) AZD5582 is a divalent AVPI motif-based Smac (DIABLO) mimetic (SMC) that acts a potent apoptosis protein repeat (BIR) domain-targeting antagonist against inhibitor of apoptosis proteins (IAPs) cIAP1/2 (BIR3 IC50 = 15/21 nM against 2.5 nM AbuRPFK-5FAM) and XIAP (BIR2/3 IC50 = 21/15 nM). AZD5582 abolishes cellular XIAP-caspase-9 interaction (1 μM, 4 hrs), induces cIAP1/2 degradation (EC50 = 0.1 nM, 1 hr) and apoptosis (GI50 <60 pM, 48 hrs) in MDA-MB-231 breast cancer cultures. AZD5582 causes substantial tumor regression by inducing cIAP1 degradation and apoptosis in tumor cells in MDA-MB-231 xenograft-bearing mice in vivo (3.0 mg/kg/wk i.v.).
SML2195 AZD6482 ≥98% (HPLC) AZD6482 is an isoform-selective and potent ATP competitive inhibitor of PI3Kb. AZD6482 produces an antithrombotic effect without an increased bleeding time or blood loss in humans and in dogs.
SML0635 AZD6765 dihydrochloride ≥97% (HPLC) AZD6765 is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist and fast-acting antidepressant. In a recent study AZD6765 relieved depression within 80 minutes, unlike most antidepressants acting on serotonin or dopamine systems which can take several weeks to work. The effects lasted from about an hour up to 2 weeks. AZD6765 has an IC50 value of 1.3 μM. Unlike more potent drugs such as ketamine, which also has rapid antidepressant activity, AZD6765 has no dissociative side-effects such as hallucinations. Earlier studies inidcated the compound has neuroprotective and anticonvulsant effects.
SML0350 AZD-7762 hydrochloride ≥98% (HPLC) AZD-7762 is a potent, ATP-competitive inhibitor of Chk1 and Chk2 that enhanced cytotoxicity DNA-damaging agents.
SML1764 AZD9272 ≥98% (HPLC) AZD9272 is a long acting, CNS penetrant, potent and selective mGluR5 antagonist.
A6850 Azelaoyl PAF 10 mg/mL in ethanol Potent PPARγ agonist.
A7611 Azelastine hydrochloride ≥98% (HPLC) H1 histamine receptor antagonist; NF-kB activator.
human ... HRH1(3269)
A7106 Azelnidipine ≥98% (HPLC), powder Azelnidipine, a novel dihydropyridine derivative, is a L-type calcium channel blocker and antihypertensive. Unlike other L-type calcium channel blockers, azelnidipine causes minimal stimulation of the sympathetic nervous system despite its significant depressor effect. Azelnidipine may have a protective role in inflammation in atherosclerosis.
A2169 3′-Azido-3′-deoxythymidine ≥98% (HPLC) Azidothymidine (AZT), a thymidine analogue, is a reverse transcriptase inhibitor against the HIV-1 virus. Azidothymidine has been shown to decrease CRISPR-mediated homology-directed repair (HDR) efficiency.
Reverse transcriptase inhibitor active against HIV-1 virus.
human ... HIVE1(3095)
mouse ... Slc29a1(63959)
SML0432 Azilsartan ≥98% (HPLC) Azilsartan is a highly potent and slowly dissociating Angiotensin II type 1 (AT1) receptor blocker (ARB) with an IC50 of 2.6 nM. It is the active form of Azilsartan medoxomil, used for treatment of hypertension. Azilsartan may also have potentially beneficial effects on metabolic syndrome including insulin sensitizing activity that may involve more than just blockade of AT(1) receptors.
human ... AGTR1(185)
SML0353 Azimilide dihydrochloride ≥97% (HPLC) Azimilide is an inhibitor of human ether-a-go-go-related gene (HERG) channel. It displays a decrease in inhibitory effect in acidic pH conditions.
Azimilide is an investigational class III anti-arrhythmic drug that blocks fast and slow components of the delayed rectifier cardiac potassium channels. It inhibits KV7.1 and KV11.1 potassium channels. Azimilide′s block of K+ currents is relatively selective for IKr over IKs: It potently blocks the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 mM), and inhibits IKs (IC50 3 mM) with nearly 10-fold less potency. At 10 mM, it does not block the inward rectifier K+ current. It blocks (10 mM) the L-type Ca2+ current (ICa) in a use-dependent manner.
75199 Azithromycin    
PZ0007 Azithromycin dihydrate ≥98% (HPLC) Azithromycin dihydrate is a macrolide antibiotic, azalide subclass. It binds to the 50S subunit of the 70S bacterial ribosomes and inhibits RNA-dependent protein synthesis in bacterial cells. Azithromycin also has anti-immunomodulatory/anti-inflammatory properties, which make it useful in treating cystic fibrosis.
Azithromycin is a non-β-lactam antibody, effective against infections associated with respiratory tract, skin, tissues and genital chlamydia. It also acts against Plasmodium falciparum and P. vivax, which are multidrug resistance species that transmit malaria. Azithromycin targets the ribosome and prevents protein synthesis. It is soluble in lipids and metabolizes in liver by undergoing demethylation.
SML2572 AZM475271 ≥98% (HPLC) AZM475271 (M475271) is an orally active, potent and selective inhibitor against src family kinases src and yes (IC50 = 25 nM & 10 nM, respectively; lck/VEGFR2/EGFR/csk/FGFR1 IC50 = 0.2/0.5/0.6/7.6/∼20 μM) that effectively suppresses src-dependent cellular signaling events (26%/48% inhibition of 50 ng/mL VEGF-induced HUVEC proliferation/migration at 100 nM; 31%/72% inhibition of 10 ng/mL VEGF-induced Flk-1/Src phosphorylation in HUVECs at 300 nM) and exbihits anticancer efficacy both in cultures (70% PC-9/30% A549 proliferation inhibition at 1 μM) and in vivo (78%/100% PC-9 tumor growth suppression in mice via 10/50 mg/kg/day p.o.).
SML0242 AZ-MTAB ≥98% (HPLC) AZ-MTAB is a potent, short acting κ-opioid receptor (KOR) selective antagonist.
PZ0038 Aztreonam ≥98% (HPLC) Aztreonam is a monobactam antibiotic used primarily to treat gram-negative bacterial infections. It is an older compound being re-examined as a therapeutic agent because of increasing carbapenem resistance in aerobic Gram-negative bacilli and because aztreonam is stable to Ambler class B metallo-β-lactamases. It is used alone or more commonly in combination with β-lactamase inhibitors such as avibactim.
SML2907 Azumolene ≥98% (HPLC) Azumolene, a more water-soluble analog of dantrolene, is a potent inhibitor of sarcoplasmic reticulum (SR) ryanodine receptor (RyR) that inhibits skeletal muscle SR Ca2+ release. Azumolene is a direct acting skeletal muscle relaxant that induces effective blockade of skeletal muscle RyR1.