Cayman Chemical

A selective CB1 receptor agonist exhibiting Ki values of 21.2 nM and >3 µM at the CB1 and CB2 receptors, respectively; more chemically stable than 2-AG, with an endogenous half-life of hours rather than minutes but 10-fold less potent than 2-AG in eliciting typical CB1-mediated responses;...

An inhibitor of the Met kinase family (IC₅₀s = 1.8, 3.9, 4.3, and 1.1 nM, respectively for Ron, Met, Tyro-3, and AxI); also inhibits Mer, FLT3, Aurora B, Lck, and VEGFR2 at higher concentrations (IC₅₀s = 14, 16, 78, 120, and 180 nM, respectively); induces polyploidy with...

An orally available, selective inhibitor of ALK (IC₅₀ = 1.9 nM) that also inhibits F1174L, R1275Q, and L1196M mutants of ALK (IC₅₀s = 1.0, 3.5, and 1.6 nM, respectively); inhibits the growth of tumors in mouse xenograft models of nonsmall cell lung cancer and anaplastic...

A major green tea polyphenol with antioxidant, anti-inflammatory, and anticancer activities.

A potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM); blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.

A potent, cell-permeable inhibitor of PDE4 (IC₅₀ = 50 values against other PDE forms being greater than 10 μM.

13-oxoODE is produced from 13-HODE by a NAD+-dependent dehydrogenase present in rat colonic mucosa. 13-OxoODE stimulates cell proliferation when instilled intrarectally in rats. 13-OxoODE has also been detected in preparations of rabbit reticulocyte plasma and mitochondrial membranes, mostly...

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to...

24(S)-hydroxy Cholesterol is a side-chain substituted oxysterol that has important roles in cholesterol homeostasis. It is generated by the action of CYP46 on cholesterol in the brain and diffuses across the blood-brain barrier to the systemic circulation where it can modulate cell signaling, be...

A water soluble prodrug analog of AEA with similar activity to that of AEA in the growth inhibition of C6 glioma cells; also a structural variant of LPA, however, its effects on the various LPA receptors have not been tested.

A potent and selective G9a HMTase inhibitor (IC₅₀ = 15 nM, Kd = 23 mM); more than 1,000-fold selective for G9a over SET7/9 and SET8.

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC₅₀s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

A cell-permeable AM ester of the fluorescent calcium indicator fluo-3.

A potent inhibitor of mPGES-1 (IC₅₀ = 16.5 nM for recombinant human enzyme); blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC₅₀s = 0.4-5 µM).

A potent Pim-1 inhibitor (Ki = 91 nM) that targets the ATP-binding kinase hinge region.

A positive modulator of the small conductance calcium-activated potassium channels SK2 and SK3 (EC₅₀s = 14 and 5.6 µM, respectively); inactive on both SK1 and IK; increases the apparent calcium-sensitivity of channel activation of SK3, changing the EC₅₀ value of calcium...

A bioisostere of 17,18-EET which is approximately 50% more effective at reducing arrhythmic contraction frequency, without affecting amplitude, when tested at 30 nM.

A metabolically stable adenosine analog that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively; anticonvulsive activity in a rat model of generalized seizures.

5,8,11-ETI is a nonselective inhibitor of lipoxygenases. It inhibits 12-LO in human platelets with an ID50 value of 24 µM. 5,8,11-ETI also inhibits A23187 and L-cysteine induced LTC4 biosynthesis in mouse mastocytoma cells with an ID50 value of 5 µM. At higher concentrations, 5,8,11-ETI...

An inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.

A potent, reversible, and cell permeable proteasome inhibitor; inhibits cell growth in B16 and IPC227F cells with IC50 values of 42 and 77 nM, respectively; inhibits NF-κB activation, sensitizing a variety of carcinoma cell lines to apoptosis.

tert-butyl p-Toluate is a synthetic intermediate useful for pharmaceutical synthesis.

A potent and selective CB1 receptor antagonist (Kis = 7.8 and 7,943 nM for CB1 and CB2, respectively); less lipophilic (log P = 5.1) and therefore more water soluble than other known CB1 receptor ligands.

Features Each vial contains a mixture of standards packaged in amber ampules purged with argon >1 ml provided at the concentration specified in the insert Designed for direct snap and inject use in mass spectrometry applications Ideally suited for method development and as a system suitability...