Cayman Chemical

An inhibitor of tBid (Kd = 20 µM), blocking the release of both cytochrome c and Smac from mitochondria; prevents apoptosis in neurons treated with glutamate or oxygen-glucose deprivation; inhibits the nuclear translocation of AIF, preventing the death of OVCAR-3 cells induced by...

A cell-permeable inhibitor of Epac1 and Epac2 (IC₅₀ = 5.9 µM for Epac2); inhibits Epac1-mediated Rap1-GDP exchange activity at 25 µM, but has no effect on PKA activity; blocks Epac-mediated phosphorylation of Akt in HEK293 cells expressing either Epac1 or Epac2.

PGA1 was first isolated as a dehydration product of the PGE1 compounds found in human semen. It has been shown to cause renal vasodilation, increased urine sodium excretion, and lowered arterial pressure in hypertensive patients. It also has growth-inhibitory activity on tumor cells; the IC50 value...

A FAHFA consisting of palmitoleic acid esterified at the 9-position of hydroxy stearic acid; significantly elevated in serum of glucose tolerant AG4OX mice; may be a bioactive lipid with roles in metabolic syndrome and inflammation.

A cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis; inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.

An orally bioavailable inhibitor of MEK1/2 (IC₅₀ = 12 nM) that inhibits ERK phosphorylation in various cancer cell lines (IC₅₀s ≥ 5 nM); efficacious in several xenograft tumor models in mice, including those bearing K-Ras or B-Raf mutations, as well as in clinical studies...

An orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC₅₀s = 10-19 nM) that displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias.

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

Guanfacine-13C,15N3 is intended for us as an internal standard for the quantification of guanfacine (Item No. 22907) by GC- or LC-MS. Guanfacine is an a2-adrenergic receptor (a2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for a2A-, a2B-, and a2C-ARs, respectively, in a radioligand binding...

An antimycotic prodrug that is converted by cytosine deaminase to 5-fluorouracil, a cytotoxic drug that inhibits viral infections and has cytotoxic effects on cancer cells.

An oxidation product of AA synthesized by human platelets and Aplaysia nervous tissue.

CAS Number: 1426152-53-5 Molecular Formula: C₁₄H₁₇N₅O₂S Formula Weight: 319.4

INDIGO’s panel of RXR reporter assays utilizes non-human mammalian cells engineered to individually express human retinoic acid receptors, RXRα (NR2B1), RXRβ (NR2B2), or RXRγ (NR2B3). INDIGO’s RXR reporter cells include the luciferase reporter gene functionally linked to...

A possible metabolite produced from EPA following epoxidation of the α-5 double bond.

A competitive inhibitor of α-galactosidase (IC₅₀ = 40 nM); binds to α-galactosidase in cells and chaperones unstable enzyme variants through the endoplasmic reticulum, allowing its movement into lysosomes.

A synthetic taurine analog with broad bactericidal and fungicidal activity; binds to the extracellular wall of bacteria, blocking adherence to epithelial and fibroblast cells; induces autophagy, apoptosis, and necrosis in human cancer cells.

6-MNA is a competitive, non-selective COX inhibitor. The Ki values for ovine COX-1 and -2 are 21 and 19 µM, respectively. The IC₅₀ values are 70 and 20 µM for human recombinant COX-1 and -2, respectively.

.DELTA.2-trans Eicosenoic acid is an α,β-unsaturated fatty acid that is a bi-product of the synthesis of .DELTA.2-cis eicosenoic acid. .DELTA.2-cis eicosenoic acid and its salts have potential medical use for treating diabetes and improving lipid metabolism. A related compound,...

An orally available, selective agonist of GPR120 (EC₅₀ = ~0.35 µm); exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body...

2-O-methyl PAF C-16 is a synthetic PAF analog which contains a methyl group, attached by an ether linkage, at the sn-2 position. Although the biological activities of 2-O-methyl PAF C-16 have not been well characterized, the C-18 analog has been shown to mediate a number of biological responses...

A thiazolidinedione that selectively activates PPARγ-1 with an EC₅₀ of 500-600 nM for both human and mouse PPARγ; exhibits low level activation of PPARα in a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα.

A potential monoacetylated derivative of the natural polyamine agmatine.

N-acetyl-2-carboxy Benzenesulfonamide is a is a structural analog of aspirin that acts as a non-selective inhibitor of COX with a COX-2 selectivity index of 0.23. In vitro studies showed that N-acetyl-2-carboxy Benzenesulfonamide is a more potent inhibitor of COX-1/COX-2 with IC50 values of 0.06...

An internal standard for the quantification of fluprostenol isopropyl ester by GC- or LC-MS.