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SML0839   AGI-5198 ≥98% (HPLC) AGI-5198 is a highly potent and selective mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
 
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.
 
SML1430 Bis-Imidazole phenol IDH1 inhibitor ≥98% (HPLC), solubility: 30 mg/mL in DMSOclear 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.
 
A2734 α5IA ≥98% (HPLC) α5IA is a selective inverse agonist for Α5 subtype of GABAA receptor with a higher intrinsic activity at the A5 subtype than other drugs. α5IA enhances cognition in laboratory animals without being proconvulsant or anxiogenic. α5IA acts as an "alcohol antagonist," markedly reducing the amnesic effect of alcohol and partially attenuating sedation, similar to Ro15-4513, but without the anxiogenic effect. α5IA offers promise as a tool to study cognitive disorders, memory function, and treatment of alcohol-related disorders.
 
I117 R(+)-IAA-94 ≥98% (HPLC), solid Potent Cl- channel blocker.
 
I5784 Ibandronate sodium salt ≥97% (NMR), solid 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.
 
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.
 
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.
 
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.
 
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 is an orally active, potent and selective KV7.2/KV7.3 (KCNQ2/Q3) channel opener that is active in rodent epilepsy models.
 
I1661 ICA-105574 ≥98% (HPLC) hERG (Kv11.1) is a voltage-gated potassium channel with important cardiovascular function. Many potential and marketed drugs bind to and inhibit hERG function, causing prolongation of the electrocardiogram QT interval, which leads to life-threatening ventricular arrhythmias. Understanding of hERG function is critical for drug discovery and development. hERG exhibits a unique bell-shaped current-voltage relationship which is a result of very rapid inactivation of the channel upon voltage activation. ICA-105574 is a small molecule activator of hERG that binds to the channel to remove inactivation, thereby increasing peak current amplitude and shortening the action potential. It also modulates activation kinetics of the channel. ICA-105574 differs in efficacy, mechanism of action, and/or binding site from other known hERG activators and enhancers. This compound is a valuable tool for furthering understanding of hERG biophysics and physiology, expecially the structural transitions that occur during inactivation.
 
SML1035   ICA-121431 ≥98% (HPLC) 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 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
 
I127 ICI 118,551 hydrochloride ≥98% (HPLC), powder 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
 
I6138 Idazoxan hydrochloride α2-adrenoceptor antagonist; I2 imidazoline receptor agonist; I1 imidazoline receptor antagonist
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
I6409 IDR-1 ≥95% (HPLC) IDR-1 is an anti-infective peptide that acts on the host to stimulate the innate immune response. IDR-1 is believed to act by enhancing monocyte chemokines, while reducing pro-inflammatory cytokines (decreased TNF and IL-6 and increased IL-10).
 
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)
BM0010 Ifetroban sodium ≥98% (HPLC) Ifetroban (BMS-180291) is a potent and selective thromboxane receptor antagonist. The IC50 for inhibition of arachadonate or U-46619-induced platelet aggregation in human plasma is 7 nM and 30 nM, respectively. Ifetroban inhibits platelet aggregation in African green monkey 100% at 3 mpk, and blocks the contractile effects of U-46619 and Ang II in rabbit renal afferent arterioles.
 
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.
 
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.
 
I5531 IIK7 solid Melatonin receptor agonist
human ... MTNR1A(4543), MTNR1B(4544)
SML0188 Ikarugamycin ≥98% (HPLC), from Streptomyces sp. Ikarugamycin, an unusual pentacyclic tetramic acid produced by Streptomyces sp., has a potent activity against the protozoan Trichomonas vaginalis with IC50 of 0.3-1.25 μg/mL. Ikarugamycin also demonstrates selective Gram positive antibacterial activity and exhibits anti-ulcer activity possibly through inhibition of Helicobacter. Ikarugamycin-induced inhibition of cholesteryl-ester accumulation reduced uptake of oxidized low-density lipoprotein (LDL) in mouse macrophages J774. Moreover, Ikarugamycin inhibits Nef-induced degradation of CD4 on Human Immunodeficiency Virus type 1 (HIV) infected T cells, thus increasing its half-life and possibly restoring some normal functions lost in the infected cells. Ikarugamycin inhibition of clathrin-coated pit-mediated endocytosis indicates it as a useful agent for studying the process of endocytosis. Ikarugamycin inhibit HL-60 cell proliferation through genotoxicity and apoptosis induction and to activated caspase by induction of intracellular rise in calcium levels and activation of p38 MAP kinase.
 
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).
 
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.
 
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.
 
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.
 
I3159 IMD-0354 ≥98% (HPLC), solid Selective IKK-2 inhibitor. Blocks IκBα phosphorylation (IC50 ~ 250 nM) and prevents the induction of NF-κB p65 nuclear translocation. Cardioprotectant, reduces IL-1β and MCP-1 production (IC50 < 1 μM) in cardiomyocytes.
 
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.
 
I7013 Imidazole-4-acetic acid sodium salt Competitive antagonist at GABAC receptors.
 
I9785 Imidazolo-oxindole PKR inhibitor C16 ≥98% (HPLC) 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.
 
I9531 Imiloxan hydrochloride >98% (HPLC), solid Selective α2B-adrenoceptor antagonist.
human ... ADRA2B(151)
I8021 L-N6-(1-Iminoethyl)lysine dihydrochloride Selective inhibitor of inducible nitric oxide synthase (iNOS).
human ... NOS2(4843)
I0160 Imipenem monohydrate ≥98% (HPLC) 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)
I5159 Imiquimod ≥98% (HPLC), solid 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.
 
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.
 
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.
 
I148   Imperatoxin A >88%, lyophilized powder Selective skeletal-type ryanodine sensitive intracellular Ca2+ channel activator found in the scorpion Pandinus
 
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 Potent inhibitor of dopamine, norepinephrine and serotonin uptake.
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)
SML0328 Indazole-Cl ≥98% (HPLC) Indazole-Cl is a selective estrogen receptor modifier (SERM), a selective ERβ agonist with > 100-fold selectivity for ERβ over Erα. In a recent study reported in Cell, Indazole-Cl, but not structurally distinct ERβ-specific ligands DPN and ERB-041, blocked the expression of proinflammatory genes in microglia and astrocytes, repressing induction of factors that promote Th17 T cell differentiation and activation. Indazole-Cl is believed to bind to the ERβ that is part of an ADIOL-ERβ-CtBP transrepression pathway that mediates recruitment of CtBP corepressor complexes to AP-1-dependent promoters, repressing genes that amplify inflammatory responses and activate Th17 T cells. In studies of experimental autoimmune encephalitis (EAE), a mouse model of Multiple sclerosis, Indazole-Cl both prevented the development of EAE when given prophylactically and caused significant improvement of EAE when provided to mice after they exhibited symptoms of disease.
 
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.
 
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.
 
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.
 
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.
 
I7378 Indomethacin ≥99% (TLC) 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.
 
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.
 
SML1911 INI-43 ≥98% (HPLC) New 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.
 
SML0623   Iniparib ≥98% (HPLC) 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%    
I0510 D-myo-Inositol 1,4-bisphosphate potassium salt from bovine brain, ≥98% (TLC) Phosphoinostol broken down from glycerophosphoinositols
 
I9261   myo-Inositol 1,3,4,5,6-pentakisphosphate ammonium salt ≥95%    
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.
 
I7012 D-myo-Inositol 1,4,5-trisphosphate potassium salt synthetic    
I141   Intralipid 20%, emulsion    
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)
I9281 5′-Iodoresiniferatoxin solid Vanilloid receptor antagonist.
 
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.
 
SML0790   Iperoxo ≥98% (HPLC) 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 Nonselective muscarinic acetylcholine receptor antagonist; bronchodilator.
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.
 
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.
 
I2286 Irbesartan ≥98% (HPLC), powder Irbesartan is an angiotensin II type 1 (AT1) receptor antagonist with anti-hypertensive activity.
 
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.
 
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 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 Soluble guanylyl cyclase activator. Possesses antitumor activity.
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.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
I6504 (−)-Isoproterenol hydrochloride β-adrenoceptor agonist; increases cytosolic cAMP.
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).
 
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) 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.
 
I6658 Isradipine ≥98% (HPLC), solid L-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.
human ... CACNA2D1(781)
SML0843 ISRIB ≥98% (HPLC) 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.
 
SML0033 Itopride hydrochloride ≥98% (HPLC) Itopride is an acetylcholinesterase (AChE) inhibitor and D2 dopamine receptor antagonist. Itopride is used as a gastroprokinetic agent.
 
I4159 ITSA-1 ≥98% (HPLC), solid ITSA-1 is a suppressor of Trichostatin A (TSA) and a molecular tool for dissecting gene regulation by distinct aceytlation events (histone and tubulin). ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC inhibitors. ITSA-1 rreverses TSA induced histone acetylation, overall deacetylation. ITSA-1 also reverses TSA induced cell cycle arrest and apoptosis. Effective range 50 μM.
 
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.
 
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.
 
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 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) 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.
 
I0161 IWR-1 ≥98% (HPLC) 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).