Cayman Chemical

A selective inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50 = 70 nM), a serine hydrolase that catalyzes the hydrolysis of 2-AG.

A potent inhibitor of CENP-E (Ki = 3.2 nM); causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines; induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.

An antiparasitic drug that, in different preparations, is effective against trypanosomes; orally available and rapidly metabolized to two active metabolites.

An epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo; its effects of remain to be determined.

A small molecule inducer of definitive endoderm from embryonic stem cells; induces the differentiation of Sox17+/FoxA2+-expressing pancreatic progenitors from human and mouse embryonic stems cells (EC₅₀ = 125.5 nM in vitro) by activating the TGF-β signaling pathway.

A first generation antihistamine which is a potent antagonist of the human H1 receptor (Ki = 11.7 nM); readily crosses the blood-brain barrier and produces diverse cognitive and psychomotor effects; also antagonizes muscarinic cholinergic receptors (Ki = 100 to 260 nM for M1 through M5).

GSH is a tripeptide (γ-glutamylcysteinylglycine) widely distributed in both plants and animals. GSH serves as a nucleophilic co-substrate to glutathione transferases in the detoxification of xenobiotics and is an essential electron donor to glutathione peroxidases in the reduction of...

Iguratimod is a disease-modifying antirheumatic drug (DMARD) and COX-2 inhibitor (IC50 = 7.7 µg/ml).{66044} It is selective for COX-2 over COX-1 (IC50 = >300 µg/ml) but also inhibits the tautomerase activity of macrophage migration inhibitory factor (MIF; IC50 = 6.81 µM).{66044,66045} Iguratimod...

JW 55 is an inhibitor of the PARP domain of tankyrases (TNKS) 1 and 2 (IC₅₀s = 1.9 and 0.83 µM, respectively). By inhibiting TNKS1/2, JW 55 stabilizes Axin2 and increases degradation of β-catenin, inhibiting the β-catenin signaling pathway (IC₅₀ = 470 nM). It...

A potent, reversible, and cell permeable proteasome inhibitor; a more effective inhibitor of chymotrypsin-like, trypsin-like, and peptidylglutamyl peptide hydrolyzing proteasome activities compared to (S)-MG132 (IC₅₀s = 0.22 versus 0.89 µM (ChTL); 34.4 versus 104.43 µM (TL);...

An Hsp90 inhibitor with an IC₅₀ value of 47 nM; induces the expression of HSP27 and Hsp72 while reducing the client proteins c-Raf, B-Raf, survivin, and PRMT5, causing cell cycle arrest and apoptosis.

A reversible, ATP-competitive inhibitor of CK1δ and CK1? (IC₅₀ = ~1 µM for both), as well as CK1α (IC₅₀ = 16 µM); at 1 µM, inhibits cytokinesis in primary mouse embryo fibroblasts; used to elucidate the role of CK1 in cells and in whole organisms.

A potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively); active in vivo and often used to evaluate the actions of adrenergic receptor agonists.

The first identified agonist for OPRM1-OPRD1 heterodimerization (EC₅₀ = 403 nM) that demonstrates selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor (EC₅₀s = 14.9, 1.1, and >40 μM, respectively).

A potent, orally bioavailable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki death proteins, like Bim, leading to apoptosis; induces apoptosis in cancer cell lines expressing mutants of β-catenin 1.

A form of stearic acid that contains a DOXYL group, creating a hydrophobic spin label.

A selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer; increases ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues; metabolized by CYP450 enzymes to active metabolites; alters cholesterol...

A quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC₅₀s range from 0.3-1 µM); inhibits PDGF-stimulated DNA synthesis (IC₅₀ = 2.5 µM) without affecting activity of the EGF receptor.

CAS Number: 851881-60-2 Molecular Formula: C₂₀H₁₇F₂N₃O2 Formula Weight: 369.4

Ins(4,5)P2 is a metabolite of Ins(1,4,5)P3 that lacks a phosphate at the 1' position. Ins(4,5)P2 formation has been reported as an intermediate in the metabolism Ins(1,4,5)P3 in GH3 pituitary cells.

A potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM); produces prolonged elevation of AEA in the brain and plasma in rats after treatment; significantly and persistently reduces inflammatory pain in rats through a CB receptor-dependent mechanism.

Oleyloxyethyl phosphorylcholine is an inhibitor of PLA2 with an IC₅₀ value of 6.2 µM for porcine pancreatic PLA2.

Immunogen: human CMKLR1 amino acids 358–371 Host: rabbit Cross Reactivity: (+) human, monkey, mouse, and rat CMKLR1 Application(s): FC, IF, and WB CMKLR1 is a GPCR relevant to the cellular chemotaxis of dendritic cells and macrophages. Chemerin, or TIG2, and Resolvin E1 are ligands for this...

Arachidonic acid leelamide is the arachidonic amide analog of leelamine. Leelamine has weak affinity for the human CB1 and CB2 receptors, exhibiting 20% displacement of [3H]-CP55940 at a concentration of 10 µM. Leelamine inhibits PDK with an IC50 value of 9.5 µM. Derivatives of leelamine...