Cayman Chemical

An orally available, selective inhibitor of LSD1 (IC₅₀ < 20 nM); targets AML stem cells.

A potent inhibitor of PKC (IC₅₀ = 2.7 nM for the rat brain enzyme).

A non-selective blocker of voltage-dependent K+-channels (Kv channels) that has greatest potency at Kv1 and Kv3 family members (IC₅₀s = 290, 590, 195, 13, 29, and 100 µM for subunits 1.1, 1.2, 1.3, 1.4, 3.1, and 3.2, respectively); also blocks Kv2 and Kv4 subunits at millimolar...

A potent and selective inhibitor of class I α-mannosidases and serves as a key inhibitor of glycoprotein biosynthesis; inhibits both human ER α-1,2-mannosidase I and Golgi class I mannosidases (Golgi α-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM, respectively;...

A minor component of the oligomycin complex that acts as an inhibitor of the mitochondrial F1FO-ATP synthase, which leads to cell death.

A cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become 'analog sensitive' (as), as compared to the wild type kinase; inhibits v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 4.2 nM versus 28 μM, respectively); used...

REV 5901 is an antagonist of cysteinyl-leukotriene receptors with a Ki value of 0.7 µM for guinea pig lung membranes. It is also an inhibitor of rat neutrophil 5-LO with an IC₅₀ value of 0.12 µM.

One of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid.

Inhibits PP1 (IC₅₀ = 1.7 μM) and PP2A (IC₅₀ = 0.2 μM) while only weakly inhibiting the activity of PP2B (IC₅₀ = 1 mM); stimulates cell cycle progression and induces premature mitosis and has been shown to be active in various cancer cell lines.

A selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC₅₀ values of 0.4 and 7 μM, respectively; inhibits proliferation of human breast cancer MCF-7 cells (10 nM) and human prostate cancer DU145 cells...

A mixed antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors (Kis = 0.14, 0.49, and 0.81 nM, respectively) that also binds to 5-HT6 (Ki = 11.7 nM); developed as a novel antipsychotic that displays 20- and 94-fold higher affinity for D2 receptors compared to haloperidol and risperidone,...

LTD4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. It is the first CysLT metabolite of LTC4. Like LTC4, LTD4-induced bronchoconstriction and enhanced vascular permeability contribute to the...

N-(diphenylmethylene) Glycine benzyl ester is a synthetic intermediate useful for pharmaceutical synthesis.

A fluorescent probe that competitively binds HDAC; demonstrates fluorescence excitation and emission maxima of 325 and 400 nm, respectively, which is quenched by 50% when bound to HDAC.

A cell-permeable inhibitor of JAK3, strongly inhibiting constitutive autophosphorylation of JAK3 in L540 cells when used at 30-50 μM; without effect on other JAK isoforms and several other kinases, including Src, Lyn, Akt, EGFR, and ERK1/2.

An inhibitor of all three PKD isoforms (IC₅₀s = 3.2, 0.6, and 0.7 μM for PKD1, PKD2, and PKD3, respectively); cell permeable, blocking the phosphorylation of PKD1 on Ser916 (an autocatalytic target) in LNCaP prostate cancer cells in response to phorbol esters (EC₅₀ = 10...

A histamine H1 receptor antagonist (Ki = 9 nM) that is effective against HCV (EC₅₀ = 44 nM), preventing viral entry into host cells.

A naturally occurring PUFA formed through a 2-carbon chain elongation of arachidonic acid; present in the adrenal glands, brain, testis, and kidney.

The NOS Activity Assay measures NOS activity by monitoring the conversion of radiolabeled arginine to citrulline. This assay is simple, sensitive, and specific for NOS activity and can be used with both crude and purified enzyme preparations. The kit includes sufficient materials and reagents for 50...

A natural alkaloid in the betel nut; an agonist of the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5; causes smooth muscle contraction; has been shown to improve learning and memory and may prove to be useful in treating dementia.

An intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.

A synthetic compound made up of the arginine-glycine-aspartate motif used to inhibit integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation; also can directly induce apoptosis by activating pro-caspase-3.

JTE-013 is a potent, selective S1P2 receptor antagonist that binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, (IC50 values >10 µM for human S1P1 and S1P3). It reverses the inhibitory effects of S1P on cell migration of vascular endothelial cells and...

A selective and potent inhibitor of PKCβ1 and PKCβ2 (IC₅₀ = 4.7 and 5.9 nM, respectively) that is effective in vivo.