Cayman Chemical

An ATP-competitive inhibitor of several CDKs as well as GSK3β.

CAS Number: 1124197-58-5 Synonyms: Diflucan-d_4; Difluconazole-d_4; Fungicon-d_4; UK 49858-d₄ Molecular Formula: C₁₃H₈D₄F₂N₆O Formula Weight: 310.3

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.

An HDAC inhibitor that selectively targets HDACs 4 and 5 (IC₅₀s = 12 and 4 nM, respectively) over other HDACs (IC₅₀s = 56, 320, 850, 880, and 1,280 for HDACs 6, 1, 11, 2, and 8, respectively); displays enhanced cytotoxic effects against human cancer cell lines, compared to SAHA...

A natural sesquiterpene lactone that reduces growth (EC₅₀ = 3-35 μM) and induces apoptosis in assorted cancer cell lines; inhibits the activation of Akt (15 μM) in endometriotic epithelial cells and STAT3 activation in THP-1 cells (EC₅₀ = 10 μM); inhibits telomerase...

A metabolite of a phosphotidylinositol ether lipid analog known to target the pleckstrin homology domain of Akt and to induce apoptosis in cancer cell lines with high levels of endogenous Akt activity.

A membrane-permeant, fluorescent Na+ indicator dye; increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm.

An internal standard for the quantification of EPEA by GC- or LC-MS.

A selective inhibitor of human collagenase-3, also known as MMP-13, producing 89% inhibition at 10 µg/ml; used to evaluate the role of MMP-13 in diverse processes.

.DELTA.17-6-keto PGF1α is the non-enzymatic hydrolysis product of PGI3. PGI3 is a COX pathway metabolite of EPA in various tissues such as seminal vesicles, lung, PMNL, and ocular tissues.

A macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,...

A potent pan-Aurora kinase inhibitor that favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM); inhibits proliferation of clear cell renal carcinoma (IC₅₀ = 2/M phase.

A selective inhibitor of JAK1 (IC₅₀ = 629 nM) that displays 30-fold selectivity for JAK1- over JAK2-dependent signaling in human whole blood; blocks IL-6/STAT1 and IL-2/STAT5 signaling in cell models and whole blood assays.

A selective, ATP-competitive inhibitor of CK2 with Ki values ranging from 0.5-1 µM.

Active enzyme for drug discovery research.

A selective agonist of β3-adrenergic receptors with Ki values of 0.43, 9.17, and 37.9 µM for β3, β2, and β1, respectively.

A coordinating solvent used to activate crystallization of chemical compounds; used in flame retardant applications, as an epoxy cure catalyst, and to produce nanostructures.

A potent, selective CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 37.9 and >10, 000 nM, respectively.

AMT is a potent, relatively selective inhibitor of iNOS with a Ki of 4.2 nM in mouse macrophages. It inhibits other isoforms of NOS, but at higher concentrations; the IC₅₀ values for rat nNOS and bovine eNOS are 34 and 150 nM, respectively.

A major arachidonic acid metabolite from the 15-LO pathway.

A specific ribonucleotide reductase inhibitor; inhibits growth of human promyelocytic leukemia HL-60 cells (IC50 = 35 µM).

An orally bioavailable, selective inhibitor of PDGFRα, PDGFRβ, and FLT3 (IC₅₀s = 11, 3.2, and 4 nM, respectively); also inhibits mutant forms of these kinases, including the D842V-containing form of PDGFR and D835Y and internal tandem duplication mutations of FLT3, at nanomolar...

A naturally-occurring but rare form of sphingosine.

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC₅₀ = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC₅₀ = 0.6 µM); shows good in vivo potency and duration of action.