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An allosteric inhibitor of oncogenic K-Ras(G12C).
Selectively and reversibly blocks MAGL activity (IC50s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis.
A potent inhibitor of PKA and PKG that shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.
An angiotensin II receptor blocker with a high affinity for the AT1 receptor (Ki = 2.7 nM) and exceptionally high bioavailability (60-80%); an insurmountable antagonist of AT1; act as a cardiovascular protective agent by effectively reducing blood pressure; also useful in treating diabetes and...
A cell-permeable purine derivative that inhibits the NADP-dependent oxidoreductase, NQO1 (Ki = 1.72 µM), to depolymerize microtubules and disrupt mitosis.
Essentially identical to AEA in its agonist binding to CB1 and CB2 receptors; binds with a Ki value of 753 nM in L cells expressing the human CB1 receptor and binds with a Ki value of 1,810 nM in AtT-20 cells expressing the human CB2 receptor.
A potent σ1 receptor antagonist.
An epoxide derivative of DHA that is generated by the action of CYP450 epoxygenases; naturally occurring in plasma and brain and spinal cord tissues and is increased following dietary supplementation with ω-3 fatty acids; a substrate of soluble epoxide hydrolase (KM = 15 µM).
A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.
A potent, selective inhibitor of HDAC6 (IC50 = 56 nM); induces acetylation of α-tubulin but not histones; enhances the cytotoxicity of the broad spectrum HDAC inhibitor SAHA against cancer cells in nude mice carrying an androgen-dependent CWR22 human prostate cancer xenograft.
Source: Fibrinogen purified from human plasma citrullinated with human recombinant PAD4 plasma Uncitrullinated Fibrinogen Mr: α chain isoform 1 (95 kDa), α chain isoform 2 (69.8 kDa), β chain (55.9kDa) and isoform γ-B chain (51.5 kDa)
A cell-permeable, reversible inhibitor of a mitochrondrial glutaminase splice variant, glutaminase C (IC50 = ~2.5 µM), which is commonly found in cancer cells; blocks transformation induced by Rho GTPases and inhibits the proliferation of cancer cell lines without affecting normal...
An aspirin-triggered lipoxin that inhibits LTB4-induced chemotaxis, adherence, and transmigration of the neutrophils with twice the potency of LXA4 demonstrating activity in the nM range.
A fluoroquinolone antibiotic widely used as an antimicrobial and immunomodulatory agent; functions by inhibiting DNA A fluoroquinolone antibiotic widely used as an antimicrobial and immunomodulatory agent; functions by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, the enzymes...
Protects the heart from transient ischemia; inhibits late sodium and potassium currents (IC50s = 3.9-16.6 µM for both) and blocks ligand binding to α1, β1, and β2 adrenergic receptors (Kis = 0.5-19.5 µM for all); inhibits fatty acid β-oxidation, activating...
The trans isomer of the 16:1 fatty acid palmitoleic acid.
A commonly used NO donor and a potent vasodilator.
A cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM); inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs.
An inhibitor of SAH hydrolase; depletes EZH2 levels and inhibits trimethylation of lysine 27 on histone H3 in acute myeloid leukemia cells in a dose-dependent manner (0.2-1 μM); increases expression of the cell-cycle regulators p21, p27, and FBXO32 leading to cell cycle arrest and apoptosis.
A short-acting, second-generation, blood-glucose-lowering agent belonging to the sulfonylurea class that increases the release of endogenous insulin; commonly used to lower blood sugar levels in type 2 diabetes (non-insulin-dependent diabetes).
Peptide Sequence: human CD36 sequence amino acids 98-114 (AKENVTQDAEDNTVSF) To be used in conjunction with Cayman’s CD36 polyclonal antibody (Catalog No. 100011) to block protein-antibody complex formation during immunochemical analysis of CD36.
An orally bioavailable inhibitor of HIF prolyl hydroxylase that increases HIF stability and action; induces an effective EPO response and stimulates non-EPO mechanisms of erythropoiesis.
A structural analog of sphingosine and a novel immune modulator; inhibits lymphocyte emigration from lymphoid organs; becomes phosphorylated by sphingosine kinase in vivo to act as a potent agonist at S1P1, S1P3, S1P4, and S1P5.
Inhibits BMP type 1 receptor-induced phosphorylation of SMAD1/5/8 (IC50 = 4.9 nM); shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively).