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SML0839   AGI-5198 ≥98% (HPLC) AGI-5198 is a highly potent and selective mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
In human chondrosarcoma cell line JJ012, AGI-5198 promotes apoptosis and G2/M cell cycle arrest. It also prevents the generation of colony in chondrosarcoma cell lines. AGI-5198 hinders the multiplication of cell and induces demethylation of H3K9me3 and H3K27me3.
SML2825 I-BET469 ≥98% (HPLC) New I-BET469 is an orally active bromodomain (BrD) inhibitor with selectivity toward a subset of bromodomain-containng proteins (BCPs) and BrDs (Kd in nM: BRD4 BrD1/2 = 1.5/2.9, BRD3 BrD1/2 = 2/2.3, BRD2 BrD1/2 = 2.3/2.8, BRDT BrD1/2 = 12/100, CREBBP = 37, EP300 = 49; Kd ≥4.8 μM toward 22 other BCPs). I-BET469 targets cellular BRD4 with high affinity (pKd = 8.3 or Kd = 5.0 nM by NanoBRET) and shows in vivo efficacy in a murine acute endotoxic shock model (1, 3, 10 mg/kg po. 30 min prior to LPS) and a chronic T cell-dependent immunization model (IgG suppression on day 14 = 24% and 65%, respectively, with 0.3 mg/kg or 3 mg/kg daily po.).
SML1272 I-BET762 ≥98% (HPLC) I-BET762 (GSK525762) is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins BRD2, BRD3 and BRD4 with IC50 values of 32.5–42.5 nM and no interaction with other bromodomain-containing proteins. I-BET mimicks acetylated histone, preventing the protein-protein interaction between acetyl-lysines and the BET reader protein. This was shown to block expression of inflammatory genes in activated macrophages and confer protection against endotoxic shock and bacterial sepsis. I-BET762 also showed potent anti-myeloma activity in vitro and in vivo.
I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression. I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.
human ... BRD2(6046), BRD3(8019), BRD4(23476), BRDT(676)
SML1430 Bis-Imidazole phenol IDH1 inhibitor ≥98% (HPLC), solubility: 30 mg/mL in DMSOclear Bis-imidazole phenol blocks D-2-hydroxyglutaric acid synthesis in cells.
bis-Imidazole phenol is a potent and cell permeable inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant R132H that inhibits D-2-hydroxyglutaric acid (2HG) production in cells. bis-Imidazole phenol binds to an IDH1 R132H allosteric site at the dimer interface containing residue involved in binding of the catalytically essential divalent cation.
I117 R(+)-IAA-94 ≥98% (HPLC), solid    
SML2335 IACS-9571 trifluoroacetate salt ≥98% (HPLC) IACS-9571 is a dimethylamine analogue.
IACS-9571 is a high-affinity, potent TRIM24/BRPF1 bromodomain (BrD) inhibitor (Kd = 1.3/2.1 nM by DiscoveRx) with good selectivity over other BrDs (BRPF2/3 Kd = 12/27 nM, BAZ2B/TAF1 BrD2/BRD4 BrD1,2 Kd = 0.4/1.8/>10 μM by DiscoveRx; ≤63% binding inhibition of 25 other BrDs at 1 μM). IACS-9571 potently blocks H3K23Ac peptide from TRIM24 BrD binding (IC50 = 7.6 nM) and displaces ectopically expressed TRIM24 PHD-BrD from endogenous histone H3 in 2-hr 5 μM SAHA-stimulated HeLa cells (IC50 = 50 nM). When adiministered in mice, IACS-9571 exhibits good pharmacokinetics and oral availability in vivo (F = 29%, 10 mg/kg p.o.).
I5784 Ibandronate sodium salt ≥97% (NMR), solid Ibandronate is a nitrogen-containing bisphosphonate (N-BP). It potentially inhibits mevalonate pathway in osteoclasts. Thus, ibandronate is effectively used to treat osteoporosis and other bone-related diseases.
Ibandronate sodium inhibits farnesyl diphosphate synthase (IC50 = 20 nM). Ibandronate sodium is also a bone resorption inhibitor. It has been investigated for in vitro anti-tumor effects, such as apoptosis induction, inhibitor of cell growth, inhibition of invasive behavior, and inhibition of angiogenesis and for its in vivo role in various cancers including breast and prostate cancers.
human ... FDPS(2224)
I5904   Iberiotoxin, recombinant from Mesobuthus tamulus ≥98% (HPLC), recombinant, expressed in E. coli Exhibits the same activity as the natural form of the toxin
The single chain peptide iberiotoxin (IbTX) is a selective and reversible inhibitor of high-conductance calcium-activated potassium channels (PK,Ca). It occurs naturally in the venom of the scorpion Buthus tamulus. IbTX also modulates the binding of charybdotoxin (CbTX) to smooth muscle sarcolemmal membranes in a non-competitive manner. IbTX is similar in size to CbTX and shares considerable sequence homology with CbTX. However, IbTX differs in its overall charge in having one fewer basic and four more acidic residues than CbTX.
SML2257 IBR2 ≥98% (HPLC) IBR2 is a cell penetrant, potent and specific RAD51 inhibitor that inhibits RAD51-mediated DNA double-strand break repair and enhances cytotoxicity of multiple anticancer agents with disparate biochemical targets including the Bcr-Abl inhibitor imatinib and multiple kinase inhibitor regorafenib. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, reduces ionizing radiation-induced RAD51 foci formation, inhibits cancer cell growth and induces apoptosis.
I0157 Ibudilast ≥99% (HPLC), solid Phosphodiesterase IV (PDE4) inhbitor. Inhibits platelet aggregation. Anti-asthma drug.
human ... PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144)
SML1452 Ibufenac ≥95% (HPLC) Ibufenac is a non-steroidal anti-inflammatory drug (NSAID) analog of ibuprofen that was withdrawn for hepatotoxicity. It inhibits cyclooxygenases COX-1 and -2 activity with IC50 values of 17.4 and 13.1 μM, respectively and > 40 μM for 5-LOX. It has been used in studies of drug-induced hepatotoxicity.
human ... PTGS1(5742), PTGS2(5743)
I4883 Ibuprofen ≥98% (GC) Cyclooxygenase (COX) inhibitor that has greater activity against COX-1 than against COX-2.
human ... ALB(213), ALOX5(240), CYP1A2(1544), CYP2C9(1559), IL8RA(3577), PTGS1(5742), PTGS2(5743)
mouse ... Alox5(11689)
rat ... Alox5(25290), Ptgs1(24693)
SML1842 Ibuprofen Arginate ≥98% (HPLC) Ibuprofen arginate is the more soluble arginate salt form of the nonsteroidal anti-inflammatory drug (NSAID) ibuprofen. Ibuprofen arginate retains the inhibitory potency against COX-2 as ibuprofen and its sodium salt, however only ibuprofen arginate is able to augment cellular NO pathway through codelivery of the NOS substrate arginine. Ibuprofen arginate, but not the sodium salt form, is shown to reverse the inhibitory effects of the cardiotoxic hormone asymmetric dimethylarginine (ADMA) and NG-nitro-L-argininemethyl ester (L-NAME) against nitric oxide synthase (eNOS & iNOS) in cultures in vitro (Murine RAW264.7 macrophages and isolated mouse & rat aorta) and effectively prevent L-NAME-induced arterial blood pressure increase in anesthetized rats in vivo (0.5 mg/kg L-NAME; 114.8 μmol/kg ibuprofen arginate, equivalent to 20 mg/kg L-Arg via femoral artery cannulation).
I9910 Ibutilide hemifumarate salt ≥98% (HPLC) Ibutilide hemifumarate salt is considered a new generation "pure" Class III antiarrhythmic agent. Ibutilide binds to and alters the activity of hERG potassium channels, delayed inward rectifier potassium (IKr) channels and L-type (dihydropyridine sensitive) calcium channels.
human ... KCNH2(3757)
I0658 IC 261 ≥98% (HPLC) Casein kinase 1 δ (CK1δ) and CK1 ε inhibitor.
human ... CSNK1D(1453), CSNK1E(1454)
SML1910   IC87201 ≥98% (HPLC) IC87201 is a potent inhibitor of the nNOS/PSD-95 protein-protein interaction that blocks NMDA-induced 3′ ,5′ -cyclic guanosine monophosphate (cGMP) production in hippocampal cultures. IC87201 exhibits analgesic properties in mice pain models. Contrary to NMDA receptor antagonists nNOS/PSD-95 protein-protein interaction inhibitors spared source memory, spatial memory, and motor function in rats.
SML1616 ICA-069673 ≥98% (HPLC) ICA-069673 has higher selectivity towards KV7.2/KV7.3 heterodimeric channels than KV7.3/KV7.5 channels. ICA-069673 is considered as a part of gating modifiers.
ICA-069673 is an orally active, potent and selective KV7.2/KV7.3 (KCNQ2/Q3) channel opener that is active in rodent epilepsy models.
SML1035   ICA-121431 ≥98% (HPLC) ICA-121431 [2,2-diphenyl-N-(4-(N-thiazol-2-ylsulfamoyl)phenyl) acetamide, a small molecule inhibitor, targets the extracellular amino acids in S2 and S3 in VSDIV (domain IV voltage sensor), which is essential for Hm1a efficacy. In humans, ICA-121431 blocks TTX-sensitive Nav1.3 sodium channels upregulated in HEK-293 cells.
ICA-121431 is a potent, selective inhibitor of the human Nav1.3 and Nav1.1 voltage gated sodium channels (IC50 = 19 nM) with little or no activity against human Nav1.5 or Nav1.7 channels.
SML0551 Icaritin ≥98% (HPLC) Icaritin enhances osteoblastic differentiation of mesenchymal stem cells (MSCs). It may have estrogen-like activities.
Icaritin is a component of Epimedium flavonoid isolated from Herba Epimedii, which enhances osteoblastic differentiation of mesenchymal stem cells (MSCs) while it inhibits adipogenic differentiation of MSCs by inhibiting PPAR-g pathway. Icaritin has no effect on MSCs proliferation. Also, icaritin potently inhibits chronic myeloid leukemia (CML) and breast cancer cells proliferation most likely by modulation of MAPK/ERK/JNK and JAK2/STAT3 /AKT signaling. As other flavonoids, icaritin may exert estrogen-like activities.
SML1134 I-CBP112 ≥98% (HPLC) I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively). I-CBP112 has little activity against other bromodomains at concentrations up to 1 mM. For full characterization details, please see I-CBP112 on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
I-CBP112 is also known as (1-[7-(3,4-dimethoxyphenyl)-9-{[(3S)-1-methylpiperidin-3-yl]-methoxy}-2,3,4,5-tetrahydro-1,4-benzoxazepin-4-yl]propan-1-one). It has the ability to induce full-length p300/CBP nucleosome acetylation. It is a competitive inhibitor of acetyl-lysine. I-CBP112 regulates transcription of key inflammatory genes.
I127 ICI 118,551 hydrochloride ≥98% (HPLC), powder ICI 118,551 has been used to treat vasomotor migraines and somatic troubles related to anxiety state.
ICI 118,551 hydrochloride is a highly selective β2-adrenoceptor antagonist.
human ... ADRB2(154)
I2536 ICI 192605 ≥98% (HPLC) ICI 192605 is a potent thromboxane A2 receptor antagonist. It inhibits platelet aggregation and can reverse the effects of vasoconstrictors such as TXA2 or PGD2. ICI 192605 can reverse vasoconstriction induced by inhibition of NO production by L-NEMA, which leads to an increase in TXA2 release.
I8283 ICI 63,197 ≥98% (HPLC) Phosphodiesterase IV (PDE 4) inhibitor
I122 ICI 204,448 hydrochloride solid κ opioid receptor agonist that does not cross the blood-brain barrier.
human ... OPRK1(4986)
I9532 Icilin ≥97% (HPLC), solid Icilin is a potent agonist at the CMR1 cold- and menthol-sensitive receptor.
SML0203 iCRT14 ≥98% (HPLC) iCRT14 belongs to the thiazolidinedione class of β-catenin-responsive transcription inhibitors. It decreases the levels of Dishevelled protein and modulates the binding of T-cell factor (TCF) to DNA. It results in consistent decrease in reduction of cell proliferation and tumor growth in colon cancer cells.
iCRT14 is a Wnt / β-catenin pathway inhibitor. It is a potent inhibitor of Catenin Responsive Transcription (CRT) reporter genes, as well as endogenous gene targets. iCRT14 also disrupts β-catenin-TCF4 interaction in a dose dependent manner, and causes G0/G1 arrest in colon tumor lines.
SML0211 iCRT3 The key mediator of Wnt signaling is the transcriptional co-activator b-catenin. In the cytoplasm, b-catenin is tightly bound to a complex that includes Axin and GSK-3b. Stimulation causes b-catenin stabilization, translocation to the nucleus and association with TCF4 to initiate transcription of responsive genes, referred to as Catenin Responsive Transcription (CRT). Virtually all Wnt-associated cancers are the result of misregulated CRT. Three inhibitors of CRT (iCRT) were identified in a screen that employed RNAi based knockdown of Axin, which stimulates CRT without affecting upstream mechanisms such as GSK activity, transduction by disheveled / frizzled, etc. These compounds are potent inhibitors of CRT reporter genes, as well as endogenous gene targets. The compounds also disrupt b-catenin-TCF4 interaction in a dose dependent manner, and cause G0/G1 arrest in colon tumor lines.
I1786 ID-8 ≥98% (HPLC) ID-8 sustains self-renewal and pluripotency of mouse embryonic stem cells (ESCs) in vitro. Stimulates proliferation at a steady rate (observed in serum-free media supplemented with 10 μM over a 30 day period).
SML1199   ID45 ≥98% (HPLC) ID45 is an activator of a PERK-Nrf2 ER stress pathway with antiviral activity against coxsackievirus B3 (CVB3), the primary cause of viral myocarditis. ID45 was found to result in host cell survival during CVB3 infection by allowing maintenance of high protein translation rates for host mRNAs and suppressing cap-independent translation initiation of CVB3 RNA. ID45 induced upregulation of Glucose related protein 78 (GRP78), an indication of ER stress, and activated PKR-like ER protein kinase (PERK) which in turn caused nuclear accumulation of response element Nrf2, leading to an increase in antioxidant response elements such as NQO1. NQO1 protects eukaryotic cap-dependent translation initiation factor eIF4GI from cleavage and degradation, facilitating cap-dependent translation initiation of host cellular mRNAs and suppressing cap-independent translation initiation of viral RNA.
I1656   Idarubicin hydrochloride solid Topoisomerase II inhibitor
human ... TOP2A(7153)
I6138 Idazoxan hydrochloride α2-adrenoceptor antagonist; I2 imidazoline receptor agonist; I1 imidazoline receptor antagonist. Idazoxan can antagonize various behaviors generated by ethanol in a preclinical setting. It possesses neuroprotective activity against spinal cord injury, resulted due to experimental autoimmune encephalomyelitis (EAE) in mouse, an animal modal of multiple sclerosis (MS).
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
I5773 IDRA 21 ≥98% Blocks the rapid desensitization of the AMPA receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
SML0756   IDT307 ≥98% (HPLC) IDT307 (APP+) is a fluorescent analogue of the dopaminergic neurotoxin MPP+ monoamine transporter substrate that fluoresces after uptake into cells. IDT307 is a substrate for the dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT). IDT307 (APP+) was found to label catecholamine neuronal cell bodies with high selectivity in midbrain and was used to investigate SERT function in lymphocytes and platelets.
I2892 Ifenprodil (+)-tartrate salt NMDA antagonist acting at the polyamine site; neuroprotective agent; α-adrenergic central and peripheral vasodilator; α2 adrenergic receptor ligand.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRINA(2907)
SML2749 iFSP1 ≥98% (HPLC) iFSP1 is a potent selective inhibitor of ferroptosis-suppressor-protein 1 (FSP1) that induces ferroptosis in cancer cells. iFSP1 strongly synergizes with GPX4 inhibitors to initiate ferroptosis in cancer cells.
I4036   IgA from human serum reagent grade, ≥95% (HPLC), buffered aqueous solution    
SML1898 Iguratimod ≥98% (HPLC) Iguratimod (T-614) is an orally active anti-inflammatory compound that inhibits NF-kappaB (NF-KB) p65 subunit (RelA) phosphorylation and nuclear translocation (30 μg/mL against 10 ng/mL TNF-α; human synovial cells) without affecting IKBα degradation.
SML2937 iHAP1 ≥98% (HPLC) New iHAP1 is a potent activator of protein phosphatase 2A (PP2A) that allosterically facilitates assembly and activation of PP2A holoenzyme complex consisting PPP2R1A, PPP2R5E (B56ε, regulatory), and PPP2CA subunits. iHAP1 induces dephosphorylation of MYBL2 transcription factor on Ser241, causing irreversible cell cycle arrest of leukemia and other cancer cells in prometaphase. iHAP1 exhibits significant antitumor activity and lack of toxicity in T-ALL xenograft mice models. Normal CD34+ HSPCs are appears to be resistant to iHAP1. iHAP1 does not inhibit dopamine receptor D2.

SML1363 IHR-1 ≥98% (HPLC) IHR-1 (inhibitor of hedgehog response 1) is a potent cell-membrane-impermeable Smo antagonist. IHR-1 blocks hedgehog induced movement of Smo into the primary cilium.
C0619 III-31-C ≥98% (HPLC), solid III-31-C is a (hydroxyethyl)urea γ-secretase inhibitor that binds to γ-secretase at the substrate docking site. DAPT, also a γ-secretase inhibitor binds to the substrate docking site as well. III-31-C is useful for the affinity isolation and characterization of the protease complex and for testing other ihhibitors that affect the γ-secretase active site. The γ-secretase complex is composed of presenilin as a catalytic component and three integral membrane proteins, nicastrin, Aph-1 and Pen-2.
SML2631 IITZ-01 ≥98% (HPLC) IITZ-01 is a cell penetrant and potent autophagy inhibitor in numerous cancer cells including breast, lung, and colon cancer cells. It significantly elevates LC3-II and SQSTM1 protein levels in starvation-induced autophagy conditions. IITZ-01 accumulates within lysosomes causing liposomal deacidification, impairment of lysosomal maturation and inhibition of lysosomal degradation. Additionally, IITZ-01 induces apoptosis through the mitochondria-mediated pathway in TNBC cells MDA-MB-231 and MDA-MB-453, while sparing normal mammary epithelial MCF10A cell.
SML1622 iKIX1 ≥98% (HPLC) iKIX1 is an antifungal agent that can re-sensitize drug-resistant Candida glabrata to azole antifungals. C. glabrata fungal infections that are resistant to azoles are an increasing problem. Drug-resistant C. glabrata most commonly contain point mutations in Pdr1 that render it active. iKIX1 acts by inhibiting the protein–protein interaction between the fungal transcription factor Pdr1 and the KIX domain of the MED15 subunit of the co-activator Mediator, thus inhibiting Pdr1-dependent gene activation of key regulators of the multidrug resistance pathway. iKIX1 reduced efflux pump gene expression and restored azole-sensitivity to PDR1 gain-of-function mutant Candida glabrata strains in plate assays. In mouse assays, combination treatment with iKIX1 and fluconazole showed significant reduction of fungal burden in mice injected with two different azole-resistant C. glabrata strains.
SML1138 IKK-16 dihydrochloride ≥98% (HPLC) IKK-16 is a selective inhibitor of IKB kinase (IKK), part of the upstream NF-KB signal transduction cascade involved in the cellular response to inflammation. IKK-16 has IC50 values of 40, 70 and 200 nM for IKKβ (IKK-2), IKK complex and IKKα (IKK-1) respectively. In a mouse sepsis model, IKK-16 reduced the multiple organ dysfunction, showing an antiinflammatory and endothelial protective effect likely mediated by inhibition of inflammation through NF-KB. IKK-16 has also been found to have some activity as an inhibitor of protein kinase D (PKD) and of multidrug resistance protein 1 (MDR1, ABCB1).
SML2322 Ilaprazole ≥98% (HPLC) Ilaprazole is a proton pump inhibitor (H+/K+ ATPase inhibitor) that suppresses acids secretion. Ilaprazole is a potent and selective inhibitor of T-cell-originated protein kinase (TOPK) that suppresses cancer growth.
I9759 Ile-Pro-Ile ≥97% (HPLC) Inhibitor of dipeptidyl peptidase IV. Inhibits entry of HIV-1 or HIV-2 into T lymphoblastoid and monocytoid cell lines.
SML0110   Ilicicolin F ≥98% (HPLC), from Verticillium hemipterigenum Ilicicolin F belongs to the ascochlorin family of molecules. Ascochlorin is an isoprenoid antibiotic produced by Verticillium hemipterigenum. Ascochlorin and its derivatives have an inhibitory effect on mitochondrial respiration by blocking the oxidation-reduction of cytochrome b through center N of the cytochrome bc1 complex. Ilicicolins have antiviral activity. They inhibit the growth of the tobacco mosaic virus, herpes simplex virus type-1(HSV-1) and newcastle disease virus.

Compounds of the ascochlorin family such as Ilicicolin F, C, D and H show a wide range of inhibitory effects on farnesyl protein transferase (FPTase) activity, and a significant inhibitory effect on the activity of testosterone-5α-reductase. Ilicicolin C and F have a moderate inhibitory activity toward the enzymes acetylcholinesterase (AChE) and β-glucuronidase and are active against Pseudomonas syringae with IC50 values of 28.5 μg/mL.

All isolated ascochlorin analogs exhibit significant antitumor and cytotoxic activities. Ascochlorin and its homologues are usable in treating and/or preventing diseases that can be relieved by the retinoid X receptor ligand-dependent signal transcriptional regulation (i.e. hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune diseases, complication of diabetes, arteriosclerosis etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet β-cells and therefore can sustain insulin productivity.
I2409 Ilmofosine ≥97% (NMR), semisolid (waxy) Protein Kinase C (PKC) inhibitor; an ether lipid derivative of lysophosphatidylcholine has antineoplastic activity in vitro and in vivo. IC50 = 560 nM. Competitive at the regulatory site of PKC. Ilmofosine is active against a variety of explanted human non-small cell lung, breast, colorectal, ovarian, renal cell cancer, and melanoma tumors in vitro at concentrations of 1-30 μg/mL.
SML1528 Iloperidone ≥98% (HPLC) Iloperidone is an atypical antipsychotic, a combined dopamine (D2) and serotonin (5HT2) receptor antagonist. Iloperidone targets a selective set of dopamine, serotonin and also norepinephrine receptor subtypes. Like similar atypical antipsychotics, Iloperidone has higher affinity for the 5-HT2A receptor (Ki < 10 nM) than for the D2 receptor (Ki = 10–100) nM). Iloperidone has high affinity for dopamine D3 (Ki < 10 nM) and lower affinity for other serotonin or dopamine subtypes. Unlike most atypical antipsychotics, Iloperidone also has high affinity for norepinephrine alpha1 receptors (Ki < 10 nM) which may contribute to the drug’s efficacy on mood and cognition.
human ... DRD2(1813), HTR2A(3356)
SML1651 Iloprost ≥98% (HPLC) Iloprost is a potent prostacyclin PGI2 analog that binds with equal affinity to human prostacyclin (Prostanoid IP) and prostaglandin EP1 receptors. Iloprost acts as a vasodilator and antihypertensive, and inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets. Iloprost dilates systemic and pulmonary arterial vascular beds and has been used clinically for pulmonary arterial hypertension (PAH), scleroderma, and Raynaud′s syndrome.
Iloprost is used to treat children with PH (pulmonary hypertension) after the surgery to clear CHD (congenital heart disease). In transplant patients, this prostacyclin analogue is used to inhibit renal dysfunction. Iloprost performs various functions like vasodilatation and cytoprotection. It has higher stability than prostacyclin.
PZ0329   ILS-920 ≥98% (HPLC) ILS-920 is a rapamycin derivative with reduced immunosuppressive activity and enhanced neuroprotective activities including efficacy in vivo stroke model. ILS-920 predominantly binds to FKBP52 with a 972-fold higher selectivity for FKBP52 vs. FKBP12 than that of rapamycin, and also binds to the β-subunit of L-type voltage dependent Ca2+ channels. This dual functionality may contribute to the compound’s efficacy in stroke models.
SML0084 IM-12 ≥98% (HPLC) IM-12 is a cell-permeable indolylmaleimide that acts as a Glycogen synthase kinase 3β (GSK-3β) inhibitor, activating downstream components of canonical Wnt signaling. IM-12 significantly increased β-catenin levels. When used to treat human neural progenitor cells, IM-12 promoted neuronal differentiation resulting in an increase of neuronal cells. It has an IC50 of 53 nM in an in vitro binding assay, compared with 92 nM for SB-216763 in the same assay condition.
SML0412 IM-54 ≥98% (HPLC) IM-54 is a cell permeable, potent and selective inhibitor of necrosis. The compound inhibits necrosis induced by oxidative stress. IM-54 does not inhibit apoptosis induced by anticancer drugs.
SML1027   Imatinib mesylate ≥98% (HPLC) Imatinib mesylate is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib is a potent inhibitor of the Bcr-Abl kinase encoded by the bcr-abl oncogene as well as receptor tyrosine kinases encoded by c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Imatinib mesylate inhibition of Bcr-Abl tyrosine kinase created by the Philadelphia chromosome abnormality found in CML decreases proliferation and enhances apoptosis in leukemias CML and ALL. Inhibition of c-kit tyrosine activity inhibits mast-cell and cellular proliferation in those diseases overexpressing c-kit such as gastrointestinal stromal tumor (GIST).
SML0022 IMB-10 ≥98% (HPLC) IMB-10 is a ligand for the αMβ2 integrin that stabilizes the binding of the integrin to endogenous ligands such as proMMP-9 and fibrinogen. IMB-10 blocks migration of lymphocyte cell lines and inhibits leukocyte infiltration in a murine thioglycolate-induced peritonitis.
IMB-10 is a thioxothiazolidine compound that inhibits the infiltration of leukocytes to the site of tumor and blocks the invasion of HSC-3 carcinoma. It modulates the host inflammatory responses and tumor progression.
SML1903 IMB5046 ≥98% (HPLC) IMB5046 is a microtubule inhibitor that has antitumor activity, overcoming multidrug-resistance. IMB5046 was cytotoxic with an IC50 range of 37 to 426 nM against multiple tumor cell lines, including some that were resistant to colchicine, vincristine and paclitaxel. IMB5046 was also active against human lung tumor xenografts. IMB5046 was found to bind to tubulin at the colchicine site, but with a different binding mode. IMB5046 inhibited tubulin polymerization, and induced G2/M arrest.
SML1945 IMB-808 ≥98% (HPLC) IMB-808 is a potent Liver X receptor α and β (LXRα/β) partial dual agonist that promotes expression of genes related to reverse cholesterol transport (including ABCA1 and ABCG1), and associated with cholesterol metabolism pathway in multiple cell lines (including ApoE). Also IMB-808 promotes cholesterol efflux from macrophages and reduced the accumulated lipids of foam cells.
I3159 IMD-0354 ≥98% (HPLC), solid IMD-0354 acts as an inhibitor by inhibiting the phosphorylation of the NF-κB (nuclear factor) and its translocation into the nucleus. It blocks IκBα phosphorylation (IC50 ~ 250 nM). Cardioprotectant, that reduces IL-1β and MCP-1 production (IC50 < 1 μM) in cardiomyocytes. IMD-0354 affects angiogenesis, which has been observed in human umbilical vein endothelial cells. It prevents tube formation and migration of the cells. In vivo studies also prove that IMD-0354 inhibits retinal vessel growth. IMD-0354 also acts as an inhibitor of Aquaporin 4 (AQP4) inhibitor (IC50 0.2μM) with no inhibitory potency to IKK-β. [4]
SML2401 Imeglimin hydrochloride ≥98% (HPLC) Imeglimin is a first-in-class oral glucose-lowering agent whose mechanism of action targets mitochondrial bioenergetics, resulting in increased insulin secretion in response to glucose, improved glucose uptake by skeletal muscle, and suppression of gluconeogenesis. Imeglimin has been shown to decrease reactive oxygen species overproduction and delay mPTP opening, preventing cell death during oxidative stress, protecting beta-cells. In an animal model, it has been shown to reduce metabolic syndrome-related diabetic cardiomyopathy.
I135 Imetit dihydrobromide ≥98% (HPLC) Potent and selective H3 histamine receptor agonist.
human ... HRH3(11255)
I2279 IMID-4F hydrochloride solid, solubility: >9 mg/mL in H2O, soluble Novel imidazoline-based K(ATP) channel blocker.
SML1821 Imidafenacin hydrochloride ≥95% (HPLC) Imidafenacin is a potent antimuscarinic agent that exhibits selectivity toward muscarinic M3 receptors with Kb of 0.317 nM. Imidafenacin is used for treating overactive bladder.
SML0148 Imidapril hydrochloride ≥98% (HPLC) Imidapril hydrochloride is a long-acting inhibitor of angiotensin converting enzyme used in the treatment of hypertension, congestive heart failure and diabetic nephropathy. It restores decreased airway sensation and bladder sensation in patients with multiple sclerosis.
Imidapril is a potent angiotensin converting enzyme inhibitor and anti-hypertensive.
I9785 Imidazolo-oxindole PKR inhibitor C16 ≥98% (HPLC) C16 exhibits a neuroprotective role in adult brain injuries.
Imidazolo-oxindole PKR inhibitor C16 is a selective inhibitor of RNA-dependent protein kinases (PKR, Eif2ak2). C16 is a first reported, potent and selective PKR inhibitor. Its inhibition effect on PKR is ATP-binding site directed. C16 specifically inhibits the apoptotic PKR/eIF2a signaling pathway without stimulating the proliferative mTOR/p70S6K signaling mechanism.
I8021 L-N6-(1-Iminoethyl)lysine dihydrochloride Selective inhibitor of inducible nitric oxide synthase (iNOS).
human ... NOS2(4843)
I0160 Imipenem monohydrate ≥98% (HPLC) Imipenem is found effective against gram positive and negative aerobes and anaerobes. Imipenem is often combined with cilastatin, to inhibit its metabolism in kidney.
Imipenem monohydrate is a broad spectrum B-lactam antibiotic. It is a member of the carbapenem class of "magic bullet" antibiotics for severe infections.
I7379 Imipramine hydrochloride ≥99% (TLC) Tricyclic antidepressant; inhibits the serotonin and norepinephrine transporters with Kis of 7.7 nM and 67 nM, respectively. Has little effect on the dopamine transporter (Ki = 25 μM).
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363), SLC6A2(6530), SLC6A4(6532)
I5159 Imiquimod ≥98% (HPLC), solid Imiquimod helps to induce the innate cutaneous immunity and the cellular arm of the adaptive immune response.
Imiquimod is a caspase 3 activator, which directly induces procaspase 3 cleavage to active caspase 3. Imiquimod induces apoptosis in vivo in basal cell carcinoma. Its anti-tumor activity is related to the induction of apoptosis. Imiquimod has anti-angiogenic, anti-inflammatory, anti-viral activities. Imiquimod also acts as an immune response modulator inducing the secretion of various cytokines and chemokines.
human ... TLR7(51284)
SML1064   IMM-01 ≥98% (HPLC) IMM-01 is an agonist of the mammalian Diaphanous (mDia)-related formins that triggers actin assembly and microtubule stabilization, serum response factor-mediated gene expression, cell-cycle arrest, and apoptosis. IMM-01 inhibits DID–DAD binding, which in turn activates mDia family of formins in cells. IMM-01 slows tumor growth in a mouse xenograft model of colon cancer.
I4034 Immepip dihydrobromide ≥97% (HPLC), powder Immepip is a H3 and H4 histamine receptor agonist. Immepip is a selective H3 agonist equipotent to (R)-α-methylhistamine and also effective in vitro and in vivo. It is devoid of side activities elicited at H1 and α2 receptors and 5-HT3 receptors.
SML2795 IMP-1700 ≥98% (HPLC) IMP-1700 is a cell-active and potent inhibitor of bacterial DNA repair that inhibits the bacterial SOS-response to DNA damage. IMP-1700 targets AddAB/RecBCD repair complex and potentiates quinolone antibiotic activity in methicillin-resistant Staphylococcus aureus.
I6659 Imperatorin ≥98% (HPLC), powder Imperatorin is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.
Imperatorin is an important bioactive furanocoumarin. It is used to treat neurodegenerative diseases. It possesses anticancer, antibacterial, anti-inflammatory and HIV replication-inhibiting activities. Imperatorin serves as an inhibitor of acetylcholinesterase (AChE) and may help in treating Alzheimer′s disease (AD) and Parkinson′s disease (PD).
SML0341 Importazole ≥98% (HPLC) Importazole is an inhibitor of importin-β transport receptors. During interphase, the transport receptor importin-β carries cargoes into the nucleus, where RanGTP releases them. Importazole somehow disrupts the importin/RAN interaction. Importazole is selective among other transporters. Compounds are imported into, but not out of, cells.
SML1812 IMR-1 ≥98% (HPLC) IMR-1 is a cell penetrant and potent inhibitor of Notch transcriptional activation complex that disrupted the recruitment of Mastermind-like 1 (Maml1) to the Notch transcriptional activation complex on chromatin. IMR-1 potently inhibits the growth of Notch-dependent cancer cell lines, and inhibits growth of patient-derived tumor xenografts. IMR-1 is hydrolyzed in vivo to acid metabolite IMR-1A.
I7160 IMS2186 ≥98% (HPLC), solid IMS2186 is an anti-proliferative and anti-angiogenic agent. Apparently IMS2186 blocks the cell cycle at G2 and inhibits the production of PGE2/TNF-α. IMS2186 inhibits cell growth in vitro in tumor cells, non-transformed fibroblasts, and retinal pigment epithelial cells. IMS2186 inhibits angiogenesis (IC50 = 0.1 μM) and cell migration. Intraocular injection of IMS2186 could be a long-lasting effective treatment for CNV (choroidal neovascularization) in AMD (age-related macular degeneration) with a reduction in scarring and related visual loss.
SML1403   IN-1130 ≥98% (HPLC) IN-1130 is a potent inhibitor of the activin receptor-like kinase ALK-5 (Type 1 TGF1β recptor). The compound inhibits phosphorylation of Smad-2 with an IC50 of 36 nM. IN-1130 inhibits renal fibrosis, and also reduces tumor volume in prostate tumor xenografts in murine models.
T133 Inactin® hydrate ≥98% (HPLC) Inactin is a long-lasting rodent anesthetic with minimal effects on cardiovascular tone and renal output.
SML0969   Inauhzin ≥98% (HPLC) Inauhzin is a cell-permeable, selective inhibitor of SirT1, which effectively reactivates p53 by inhibiting SIRT1 activity. Inauhzin inhibits cell proliferation, induces senescence, and p53-dependent apoptosis of human cancer cells without apparent toxicity to normal cells.
I119 Indatraline hydrochloride solid Indatraline is a non-selective monoamine transport inhibitor. It inhibits the reuptake of neurotransmitters, such as serotonin, norepinephrine and dopamine. It exhibits anti-depressant and anti-angiogenic effects. Indatraline also plays a role in inducing autophagy.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
SML0189   Indinavir sulfate salt hydrate ≥98% (HPLC) Indinavir sulfate is an antiviral HIV protease inhibitor.
Indinavir sulfate suppresses the replication of HIV and is an important component of antiretroviral therapy for initial treatment of HIV infection. It is known to cause renal and urologic toxicity.
SML3009 Indiplon ≥98% (HPLC) New Indiplon (NBI 34060) is an orally active, high-affinity GABAA receptor positive allosteric modulator (PAM) with preferential labeling of alpha1 subunits-containing receptors (rat cerebellar/cerebral cortex membranes binding KD = 1.01/0.45 nM). Indiplon potentiates GABA-induced chloride conductance of cultured rat cortical neurons (EC50 = 11.6 nM vs 152 nM/630 nM) and exhibits sedative efficacy in mice (ED50 = 1 mg/kg/passive avoidance & 2.7 mg/kg/locomotor activity inhibition po.) and rats (ED50 = 2.5 mg/kg/locomotor activity inhibition & 3 mg/kg/vigilance impairment po.) in vivo. Indiplon shows greater affinity, in vitor and in vivo potency than zaleplon and zolpidem.
SML0280 (2′Z)-Indirubin ≥98% (HPLC) Indirubin is an inhibitor of GSK-3β and of cyclin-dependent kinases (CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, CDK5/p35). Also, indirubin is a specific Aryl Hydrocarbon receptor (AHR) ligand.
I0404 Indirubin-3′-oxime ≥98% (HPLC), solid Indirubin-3′-oxime is a cyclin-dependent kinase inhibitor which functions by competing with ATP for binding to the catalytic subunit; exhibits antiproliferative activity leading to G2/M arrest in many cell lines and G1/S arrest in Jurkat cells.
Indirubin-3′-oxime mediates apoptosis in Jurkat T cells and has anti-tumor functionality. Indirubin-3′-oxime inhibits Y box binding protein 1 (YB1) translocation, contributing to anticancer functionality. Indirubin-3′-oxime decreases expression of estrogen-related receptor γ (ERRγ) and peroxisome proliferator-activated receptor-γ co-activator-1α (PGC1α) in human neuroblastoma, leading to cell cycle arrest and mitochondrial dysfunction.
SML1225 Indisulam ≥98% (HPLC) Indisulam is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.
Indisulam is synthetic sulfonamide compound. In vitro and in vivo studies point out that indisulam prevents retinoblastoma protein phosphorylation. Also, it inhibits cyclins A and B1 activity. Indisulam is known to promote apoptosis. Indisulam is a potent inhibitor of cellular dehydrogenases and thus, is likely to interfere with metabolic pathways such as malate-aspartate shuttle, glycolysis and gluconeogenesis.
I0661 (−)-Indolactam V ≥96% (HPLC) (-)-Indolactam V is a PKC activator shown to effect differentiation in embryonic stem cells leading to development of pancreatic precursors. It is active in the mouse model.
(−)-Indolactam V is naturally present in Streptoverticillium blastmyceticum. It serves as a precursor to the teleocidin class which are alkaloids. It is a the pharmacophore of lyngbyatoxin and teleocidins.
I7378 Indomethacin 98.5-100.5% (in accordance with BP) Cyclooxygenase (COX) inhibitor that is relatively selective for COX-1.
human ... ALB(213), ALOX5(240), ELA2(1991), GPR44(11251), IL1A(3552), PLA2G1B(5319), PTGDR(5729), PTGS1(5742), PTGS2(5743)
mouse ... Alox5(11689), Ptgdr(19214), Ptger1(19216), Ptger2(19217), Ptger3(19218), Ptger4(19219), Ptgs1(19224)
rat ... Alox5(25290), Ptgs1(24693), Ptgs2(29527)
I7904 Indomethacin heptyl ester methyl acetate solution, ≥98% (HPLC) Potent cyclooxygenase-2 inhibitor. 1700 times greater activity against COX-2 than COX-1.
I2909 Indoramin hydrochloride ≥98% (HPLC), solid α1-adrenoceptor antagonist.
SML1011   INDY ≥98% (HPLC) INDY is a potent inhibitor of Dyrk1A and Dyrk1B (dual-specificity tyrosine-phosphorylation-regulated kinase 1). The IC50 values for inhibition of Dyrk1A and 1B are 240 and 230 nM, respectively. INDY impairs the self-renewal capacity of neural stem cells and glioblastoma tumor-initiating cells.
SML2239 INF39 ≥98% (HPLC) INF39 is an orally active acrylate derivative and a non-cytotoxic INF4E analog (no toxicity at 100 &mu;M in THP-1 cultures vs. TC50 = 65 &mu;M with INF4E) that acts as an irreversible inhibitor against NLRP3 (NACHT, LRR and PYD domains-containing protein 3) ATPase activity (52% inhibition in 15 min by 100 &mu;M INF39; 105 ng human NLP3 & 250 &mu;M ATP) essential for the NLRP3 inflammasome assembly and activation. INF39 effectively decreases 5 mM (30 min) ATP-induced interleukin-1β (IL-1β) release and pyroptosis of murine bone marrow-derived macrophages in cultures (by 55-58% and 43-65%, respectively, with 1-hr 10 &mu;M INF39 pretreatment of LPS-primed BMDM) and alleviates gut-associated inflammation in a rat model of 2,4-dinitrobenzenesulfonic acid (DNBS)-induced colitis in vivo (12.5-50 mg/kg/day in 0.2 mL olive oil p.o.).
SML1318 Ingenol-3-angelate ≥95% (HPLC) Ingenol 3-Angelate is a diterpenoid ester isolated from Euphorbia peplus that induces rapid cell death with keratinocytes and some cancer cell lines. Ingenol 3-Angelate is a protein kinase C activator that displays potent antileukemic activity. Ingenol 3-Angelate (ingenol mebutate) is used for treatment of actinic keratosis.
Ingenol-3-angelate, is a phorbol ester-like compound or a diacylglycerol analog that is used in the treatment of several disorders like skin cancer. It is also known as PEP005. Ingenol-3-angelate stimulates the initiation of the enzyme by providing PKCs (protein kinase C) to cellular membranes.
SML1911 INI-43 ≥98% (HPLC) INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as that of its cargo transcription factors, NFY, AP-1, p65, and NFAT. INI-43 exhibit specific cytotoxicity toward cancer cells. INI-43 inhibits tumor growth in cancer xenograft models.
INI-43 is also known as (3-(1H-benzimidazol-2-yl)-1-(3-dimethylaminopropyl)pyrrolo[5,4-b]quinoxalin-2-amine). It has the ability to prevent the development of dermatologically xenografted esophageal and cervical tumor cells. INI-43 can also decrease activator protein 1 (AP-1) transcriptional activity, induced by phorbol-12-myristate-13-acetate (PMA).
SML0623   Iniparib ≥98% (HPLC) 4-iodo-3-nitrobenzamide, the intracellular metabolite of iniparib has the capability to covalently prevent PARP1 (poly(ADP-Ribose) polymerase 1) under cell-free conditions. PARP inhibitor also plays a role in BRCA (breast cancer susceptibility protein) deficient tumors.
Iniparib (BSI-201) is an antineoplastic originally thought to be a poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. Recent studies indicate Iniparib is not a PARP-1 inhibitor, and its mechanism of action is currently unknown.
I5125 myo-Inositol ≥99% A component of membrane phospholipids, glycosyl­phosphatidyl­inositol anchors that bind glycoproteins to cell membranes, and inositol phosphate second messengers.
I8132 scyllo-Inositol ≥98%    
I8636 D-myo-Inositol 1,3,4,5-tetrakis(phosphate) ammonium salt ≥95% Precursor of inositol 1,3,4-trisphosphate; increases entry of calcium across the plasma membrane; proposed regulator of intracellular calcium by control of plasma membrane transport of calcium ions.
SML2918 INT131 ≥98% (HPLC) INT131 is a brain penetrant, non-thiazolidinedione, highly potent and selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator (SPPARM) that displays anti-diabetic activities. INT131 is a partial, rather than a full agonist of PPARγ, and in clinical trials has shown increased glucose tolerance without the weight gain and cardiovascular side effects seen with some of the full agonist.
I141   Intralipid 20%, emulsion Intralipid is a lipid emulsion comprising soybean oil. It favors proinflammatory cytokines production and is recommended for the treatment of immune-mediated pregnancy and implantation failure. In parenteral nutrition, intralipid is the source of fats. It elicits protection in heart ischemia-reperfusion injury by inhibiting mitochondrial permeability transition pore opening. Intralipid is an effective alternative for intravenous immunoglobulin and improves bioavailability of platinum based anti-cancer drugs.
SML2630 Intronistat B hydrobromide ≥98% (HPLC) Intronistat B is a potent inhibitor of the self-splicing group IIB intron, a mitochondrial RNA tertiary structure necessary for respiration in fungi, yeast and plants, but not found in vertebrates. Intronistat B was found to have antifungal activity comparable to that of amphotericin B in inhibiting growth of the Candida parapsilosis. It did not inhibit spliceosomal processing, group I intron splicing or splicing of group II introns from subclasses other than subclass IIB and was not toxic to human cells.
SML1850 Inz-1 ≥98% (HPLC) Inz-1 is a potent and selective inhibitor of yeast mitochondrial cytochrome bc1 that reverses resistance to triazole antifungals in the pathogenic fungus Candida albicans.
SML0023 5-Iodo-A-85380 dihydrochloride hydrate ≥98% (HPLC) 5-Iodo-A-85380 increases the influx of extracellular Ca+2 in rat cortical neurons and exhibits protective effects against glutamate-induced neurotoxicity. Studies reveal that it also activates α6β2 nicotinic acetylcholine receptors.
5-Iodo-A-85380 is a highly selective α4β2 nicotinic receptor agonist. The Ki values for binding to the human and rat receptors are 12 and 10 pM, respectively.
I1757 19-Iodo-5-androstene-3β-ol-17-one 3-acetate    
I9890 m-Iodobenzylguanidine hemisulfate salt ≥98% (HPLC and TLC) Antitumor agent which inhibits ADP ribosylation.
I8255 19-Iodocholesterol 3-acetate ~95% (TLC)    
I0909 6-Iodonordihydrocapsaicin ≥98% (HPLC), solid TRPV1 (V1) vanilloid receptor antagonist.
human ... TRPV1(7442)
I7033 6′-Iodoresiniferatoxin amorphous semi-solid VR1 vanilloid receptor partial agonist.
SML0645   Iomazenil ≥98% (HPLC) Iomazenil (Ro 16–0154) is a benzodiazepine competitive antagonist and partial inverse agonist. Iomazenil has been shown to counteract the effects of alcohol.
I0634 Ionomycin calcium salt from Streptomyces conglobatus powder, ≥98% (HPLC) Ca2+ ionophore that is more effective than A23187 as a mobile ion carrier for Ca2+; non-fluorescent; used to study Ca2+ transport across biological membranes; induces apoptotic degeneration of embryonic cortical neurons.
SML0652 IOX2 ≥98% (HPLC) IOX2 is selective and potent inhibitor of prolyl hydroxylases (PHD). Stabilization of HIF-1R through inhibition of PHD has been examined as a potential treatment for ischemic diseases including anemia, myocardial infarction, and stroke. IOX2 is a selective inhibitor of the hypoxia inducible factor (HIF) prolyl-hydroxylases (PHD) that exhibits up-regulation of HIF1a in zebrafish. For full characterization details, please visit the IOX2 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
I2285 IPA-3 ≥95% (HPLC), powder IPA-3 is an allosteric inhibitor of Pak1. It binds to autoinhibitory domain of Pak1 (p21 activated kinase), highly selective amongst kinases. Pak1 is implicated in tumorigenesis and metastasis.
SML1322   Ipamorelin acetate ≥98% Ipamorelin is a selective growth hormone secretagogue and agonist of the ghrelin receptor that selectively stimulates the ghrelin receptor and causes growth hormone release. The potency and efficacy of ipamorelin are similar to GHRP-6 but without increase plasma levels of ACTH or cortisol. Ipamorelin appears to enter the central nervous system and to activate GRLN receptors in the spinal cord.
Ipamorelin is known to be useful in reducing the symptoms of postoperative ileus is a gastrointestinal dysfunction arising due to abdominal surgery. Symptoms include abdominal distention, vomiting, nausea, constipation and anorexia.
SML0790   Iperoxo ≥98% (HPLC) Iperoxo forms an important building block for the class of G protein-coupled receptors modulators. Iperoxo specifically binds to the orthosteric site of the muscarinic acetylcholine receptor. It has a higher efficacy than the endogenous agonist acetylcholine.
Iperoxo is a muscarinic acetylcholine receptor superagonist. The pEC50 values for G-protein activation by acetylcholine and iperoxo in CHO cells expressing recombinant human M2 receptors are 7.6 and 10.1, respectively.
SML0472 4-IPP ≥97% (HPLC) 4-IPP is a cell permeable, potent macrophage migration inhibitory factor (MIF) antagonist that covalently modifies MIF N-terminal proline.
I1637 Ipratropium bromide monohydrate ≥98% (TLC), powder Ipratropium bromide monohydrate is a nonselective muscarinic acetylcholine receptor antagonist and a bronchodilator. In nebulized form, it is used for treating asthma and obstructive pulmonary diseases. It acts as a β2 adrenoreceptor agonist. Ipratropium bromide monohydrate is an anticholinergic agent and competes with acetylcholine. It promotes bronchodilation by stimulating sympathetic pathways.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
SML1147 IQ-1 ≥95% (HPLC) IQ-1 enhances β-catenin/CBP interactions and blocks β-catenin/p300 driven transcription, which enables mouse embryonic stem cells (ESCs) to be maintained in an undifferentiated pluripotent state, allowing expansion and self-renewal of mouse ESC populations.
SML0605   IQ-1S ≥98% (HPLC) IQ-1S is an inhibitor of JNK kinases, with a preference for JNK3. Kd values for IQ-3 binding to JNK 1, 2 and 3 binding are 390, 360 and 87 nM, respectively. The compound inhibits JNK phosphorylation and NFkB /AP-1 transcriptional activity in human monocytic cells at low mM concentrations, and inhibits CD4+ T-cell immune response in a murine delayed-type hypersensitivity (DTH) model.
SML2138 IR415 ≥98% (HPLC) HBx is a viral suppressor of host defenses consisting of RNAi-based silencing of viral genes. It is important for HBV replication and also functions as an RNAi suppressor protein. HBx is considered as emerging target for anti-viral therapy.
selective inhibitor of Hepatitis B Virus X Protein (HBx)
I5409 IRAK-1/4 Inhibitor I ≥98% (HPLC), solid IRAK-1/4 Inhibitor I is a novel benzimidazole that is a potent inhibitor of interleukin-1 receptor-associated kinases 1/4 (IRAK 1/4). IC50 values were 300 nM and 200 nM for IRAK-1 and -4, respectively, and >10,000 nM for a panel of 27 other kinases tested.
IRAK1 overexpression leads to the development of head and neck squamous cell carcinoma (HNSCC). Therefore, IRAK-1/4 inhibitor I might be a potential therapeutic for HNSCC tumors. Various experimental studies states that IRAK-1/4 inhibitor might have a potential to exhibit inhibitory effects on the nuclear factor (NF)-κB signaling pathway.
I2286 Irbesartan ≥98% (HPLC), powder Irbesartan is an angiotensin II type 1 (AT1) receptor antagonist with antihypertensive activity. It also elicits selective peroxisome proliferator-activated receptor γ (PPARγ)-modulating activity and possesses anti-inflammatory properties. Irbesartan shows protective cardiovascular effects and provides protection against chronic glomerulonephritis.
human ... AGTR1(185)
SML1521 Irsogladine maleate ≥98% (HPLC) Irsogladine maleate is an inhibitor of phosphodiesterase 4 (PDE4) with gastroprotective activity. Irsogladine maleate is a mucosal protective drug with a number of activites including facilitation of gap junctional intercellular communication, inhibition of the reduced gastric mucosal blood flow response, and suppression of reactive oxygen species (ROS) production.
SML1902 ISAM-140 ≥98% (HPLC) ISAM-140 is a potent and selective A2B adenosine receptor antagonist (A2BAR). ISAM-140 exhibits remarkable selectivity over A1, A2A, and A3 adenosine receptors.
SML2357 Isavuconazole ≥98% (HPLC) Isavuconazole is a triazole antifungal drug. It inhibits fungal sterol biosynthesis by inhibition of cytochrome P450 sterol 14-α-demethylase (CYP51), an enzyme in the sterol biosynthesis pathway that leads from lanosterol to ergosterol. It has been approved for the treatment of both invasive aspergillosis and invasive mucormycosis.
I6410 ISCK03 ≥98% (HPLC), solid ISCK03 inhibits in vitro phosphorylation of c-Kit in a dose dependent manner. ISCK03 inhibits SCF (stem cell factor)-induced c-kit phosphorylation in 501mel human melanoma cells. Complete inhibition was observed with 1 and 5 μM ISCK03.
SML1450 Isobavachalcone ≥98% (HPCE) Isobavachalcone is a chalcone isolated from multipurpose medical plant Psoralea corylifolia that inhibits LPS-induced ICAM-1 expression and leukocyte adhesion to brain endothelial cells. It appears that isobavachalcone modulates both MyD88-dependent and TRIF-dependent signaling of toll-like receptor 4 (TLR4). Isobavachalcone significantly inhibits both oligomerization and fibrillization of Aβ42. Isobavachalcone exhibits a wide spectrum of biological activities including antioxidative, antiplatelet, antimicrobial, anti-inflammatory, antitumor, and neuroprotective.
I3639 Isoetharine mesylate salt β-Adrenergic receptor agonist; bronchodilator.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
G002 Isoguvacine hydrochloride solid Isoguvacine is a strong γ-aminobutyric acid A (GABAA) receptor agonist.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
I3766 Isoliquiritigenin powder Isoliquiritigenin is a soluble guanylyl cyclase activator and possesses antitumor activity. It also possesses antioxidant, antiplatelet and estrogenic properties.
rat ... Alox5(25290)
I1282 Isopentenyl triphosphate ammonium salt solution ≥95% (TLC) Isoprenoid building block.
I6783   Isopimaric Acid ≥98% (GC), powder Potent opener of large conductance calcium activated K+ (BK) channels.
I5627 Isoprenaline hydrochloride β-adrenoceptor agonist; increases cytosolic cAMP.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
I0763 N9-Isopropylolomoucine ≥98% (HPLC) Inhibitor of certain cyclin-dependent kinases; increased potency in some systems over olomoucine.
I2760 (−)-Isoproterenol (+)-bitartrate salt powder β-Adrenoceptor agonist; increases cytosolic cAMP.
Isoproterenol functions as an ovine pulmonary vein dilator.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
I6504 (−)-Isoproterenol hydrochloride β-adrenoceptor agonist; increases cytosolic cAMP.
Isoproterenol hydrochloride is useful in post transplantal organ recovery. It exhibits ionotropic and chronotropic effects. With respect to donor heart recovery, isoproterenol hydrochloride decreases peripheral and systemic vascular resistance. Isoproterenol also increases the heart rate.
human ... ADRB2(154)
I138 1,5-Isoquinolinediol ≥98% (HPLC), powder DiQ is a potent inhibitor of Poly(ADP-ribose) synthetase which is activated by nitric oxide; neuroprotective agent.
SML0590 Isorhapontigenin ≥98% (HPLC) Isorhapontigenin or 4-methoxyresveratrol is a stilbene derivative isolated from a number of plants including Chinese medical herbs Gnetum Cleistostachyum and Iris Domestica (Belamcanda chinensis, leopard lily), and wine grapes. Similarly to resveratrol, isorhapontigenin is a potent antioxidant that attenuates ROS generation. Also, Isorhapontigenin exhibits pro-apoptopic and anti-cancer activities through downregulation of XIAP (X-linked inhibitor of apoptosis protein).
SML2383 Isosilybin ≥98% (HPLC) Isosilybin is a diastereoisomeric mixture of flavonolignans isosilybin A and isosilybin B isolated from milk thistle (Silybum marianum) that exhibits hepatoprotective activity. Isosilybin potently inhibits Cytochrome P4502C8 (CYP2C8) activity in human liver microsomes. Also Isosilybin is an activator of PPARγ.
PZ0331 ISOX-DUAL ≥98% (HPLC) ISOX-DUAL is a potent dual inhibitor of the bromodomain of CREB binding protein (CBP BRD) and bromodomain-containing protein 4 (BRD4).
PZ0332 ISOX-INACT ≥98% (HPLC) CBP BRD (CREB binding protein bromodomain) inhibition serves as an effective therapeutic target for Parkinson’s disease. The inhibition is followed by negative regulation of a number of macrophage inflammatory genes. It also downregulates G-protein signaling 4 mRNA.
ISOX-INACT is an inactive control probe for the highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) PF-CBP1.
SML0523   ISPA-28 ≥98% (HPLC) ISPA-28 is an inhibitor of the plasmodial surface anion channel (PSAC). ISPA-28 is 800 fold more potent against PSAC expressed by the P. falciparum strain Dd2 over PSAC expressed by the HB23 strain. PSAC is incorporated into the membranes of Plasmodium-infected red blood cells, resulting in increased permeability to nutrients required for pathogen growth.
SML2869 Ispinesib ≥98% (HPLC) Ispinesib (SB-715992) is a potent and highly selective kinesin spindle protein (KSP, KIF11, EG5) allosteric inhibtor that specifically inhibits microtubule (MT)-stimulated ATPase activity of KSP (Ki = 1.7 nM; 5 μM MT, 500 μM ATP, 0.75 nM human KSP), but not ubiquitous kinesin heavy chain KHC, neuronal kinesin KIF1A, or mitotic kinesins CENP-E, RabK6, MCAK, MKLP1. Ispinesib exhibits anti-cancer efficacy in cultures (GI50 = 45 nM/BT-474 & 19 nM/MDA-MB-468) and in cancer xenograft models in vivo (8 or 10 mg/kg q4d×3 ip. mice with MCF-7, HCC-1954, KPL4, BT-474 xenografts).
I6658 Isradipine ≥98% (HPLC), solid Isradipine is considered as an active calcium channel blocker, used to treat hypertension.
L-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.
human ... CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), CACNA2D1(781)
SML0843 ISRIB ≥98% (HPLC) ISRIB (integrated stress response inhibitor) as a drug, imparts resistance to the cells against the downstream effects of eukaryotic initiation factor 2 (eIF2)α phosphorylation such as activating transcription factor 4 (ATF4) and eukaryotic translation initiation factor 4E (eIF4E)-binding protein 1 (4E-BP1) induction.
ISRIB is a blood- brain barrier penetrant, potent and selective inhibitor of integrated stress response (ISR) that impairs adaptation to ER stress. ISRIB is a potent inhibitor of PERK signaling, which potently reverses the effects of eIF2a phosphorylation and restores the cells translation capacity. ISRIB enhances cognitive memory in rodents.
SML0422 Istradefylline ≥98% (HPLC) Istradefylline (KW-6002) is a potent and selective adenosine A2A receptor selective antagonist which has been investigated for use in Parkinson′s Disease.
human ... ADORA2A(135)
SML1947 ITH12575 ≥98% (HPLC) ITH12575 is apotent and selective inhibitor of mitochondrial Na+/Ca2+ exchanger mNCX with neuroprotective activity. It was shown to reduce Ca2+ efflux from the mitochondria to the cytosol with an EC50 value of 690 nM and was shown to protect against Ca2+ overload and mitigated the neuronal damage in a model of oxidative stress. At higher concentrations ITH12575 also reduced Ca2+ influx through CALHM1, a Ca2+ channel that plays a key role in the neuronal electrical activity.
SML2669 ITK7 ≥98% (HPLC) ITK7 is a cell penetrant, potent and selective inhibitor of PARP11 mono-ADP-ribosylation (MARylation) activity.
SML0033 Itopride hydrochloride ≥98% (HPLC) Itopride hydrochloride enhances the gastrointestinal motility by blocking the activity of dopamine on the D2 receptors, on the post-synaptic cholinergic nerves and by inducing the liberation of acetylcholine in the myenteric plexus. It also inhibits the hydrolysis of the released acetylcholine with the help of acetylcholinesterase.
Itopride is an acetylcholinesterase (AChE) inhibitor and D2 dopamine receptor antagonist. Itopride is used as a gastroprokinetic agent.
I1411 ITX3 ≥98% (HPLC) ITX3 is a specific inhibitor of endogenous TrioN activity acting on the GEF domain and selective cell active inhibitor of the Trio/RhoG/Rac1 pathway. The compound is active in whole cell assay where it inhibits the formation of TrioN-dependent cell structures. ITX3 appears to be specific for TrioN inhibition rather than other RhoGEFs.
I1911 IU1 ≥98% (HPLC) IU1 is an inhibitor of USP14, a deubiquitinating enzyme associated with the proteasome. The proteasome mediates the cellular degradation of oxidized, damaged and misfolded proteins which, if not removed, accumulate and become toxic to cells. Proteins targeted for proteasomal degradation are first ubiquitinated, with longer length ubiquitin chains interacting more strongly with the proteasome. Deubiquitinating enzymes (DUBs) such as USP14 interfere with the degradation process. IU1 inhibits USP14-mediated ubiquitin "chain-trimming" thereby enhancing substrate degradation by the proteasome. The compound may help to eliminate toxic proteins more effectively by enhancing their degradation.
SML2240 IU1-47 ≥98% (HPLC) IU1-47 is a potent and selective inhibitor of the deubiquitinating enzyme UPS14. IU1-47 enhances protein degradation including human wild-type and pathological Tau forms in neurons.
SML0281 Ivabradine hydrochloride ≥98% (HPLC) Ivabradine hydrochloride is an open channel blocker of neuronal I(h) and related cardiac I(f) channels, which are comprised of subunits of the hyperpolarisation-activated cyclic nucleotide-gated (HCN) channels, in particular HCN4. Ivabradine has antianginal activity. It lowers heart rate and reduces myocardial oxygen demand.
Ivabradine is used to treat chronic heart failure.
human ... HCN4(10021)
I8898 Ivermectin Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptor; also modulates glutamate-GABA-activated chloride channels.
human ... ABCB1(5243), CYP3A4(1576)
mouse ... Abcb1a(18671), Abcb1b(18669)
I0536 IWP-2 ≥98% (HPLC) IWP-2 is an inactivator of Porcn function; inhibitor of Wnt production. Wnt/b-catenin (‘canonical’) pathway maintains transcriptional programs that enable stem cells to remain multipotent. Hyperactivation of the Wnt/b-catenin pathway leads to disease stage. IWP-2 inhibits Wnt production. It appears that IWP inactivates Porcn function either by directly inhibiting the Porcn active site or by modulating the function of a Porcn regulator. Porcn is a member of the membrane-bound O-acyltransferase (MBOAT) family, which adds a palmitoyl group to Wnt proteins that is essential to their signaling ability and is required for Wnt secretion. IWP-2 is useful in both regenerative medicine and anticancer efforts.
SML0533 IWP-3 ≥98% (HPLC) IWP-3 is a Wnt inhibitor that prevents palmitylation of Wnt proteins by Porcupine (Porcn). IWP-3 is an inactivator of Porcn function that acts as inhibitors of Wnt production. Studies revealed that IWP-3 induces differentiation of human mesoderm cells to form cardiomyocytes.
SML1114 IWP-4 ≥95% (HPLC) IWP-4 blocks Wnt family member 5a. It blocks Wnt protein secretion and prevents the canonical and non-canonical signaling pathways.
IWP-4 is a potent inhbitor of the Wnt pathway regulatory protein porupine (Porcn). IWP-4 blocks palmitylation, and subsquent secretion and activity of Wnt. IWP-4 induces the differentiation of human pluripotent stem cells into cardiomyocytes.
SML0677   IWP12 ≥98% (HPLC) IWP (inhibitor of Wnt production) inhibitors are known to prevent Wnt protein generation. Abnormal Wnt signalling associated with tumorigenesis and metastasis of tumors.
IWP12 is Wnt inhibitor that prevents palmitylation of Wnt proteins by Porcupine (Porcn), which is suitable for in vivo assays. IWP12 blocked post resection juvenile zebrafish tailfin regeneration.
SML1962   IWP-O1 ≥98% (HPLC) IWP-O1 is an inhibitor of Porcupine (Porcn), an acyl (palmitoyl) transferase essential for secretion of Wnt proteins and involved in both embryonic development and tumor progression. IWP-O1 has good metabolic stability and is extremely potent, exhibiting an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling.
I0161 IWR-1 ≥98% (HPLC) IWR-1 is a tankyrase inhibitor and is cytotoxic for cancer stem-like cells. It inhibits the in vivo progression of osteosarcoma. IWR-1 interacts with RNA polymerase II and is crucial for the formation of preinitiation complex.
The Wnt/b-catenin (‘canonical’) pathway maintains transcriptional programs that enable stem cells to remain multipotent. Hyperactivation of the Wnt/b-catenin pathway leads to disease stage. IWR-3 act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b).
SML2615 Ixabepilone ≥98% (HPLC) Ixabepilone is a microtubule stabilizing semisynthetic lactam analog of epothilone B. It appears that Ixabepilone is unaffected by BCRP mediated chemoresistance.