19 products were found matching "Cay16210"!

5-trans PGF2alpha is the more thermodynamically stable C-5 olefin isomer of PGF2alpha and is a common impurity in commercial lots of PGF2alpha. 5-trans PGF2alpha administered intravenously to anesthetized rabbits caused a substantial (ten-fold) increase in respiratory rate, but this attribute was common to a number...

Pellitorine is an amide alkaloid that has been found in P. nigrum and has diverse biological activities. Pellitorine is cytotoxic to HL-60 leukemia and MCF-7 breast cancer cells (IC50s = 13 and 1.8 µg/ml, respectively). It inhibits production of TNF-alpha, IL-1alpha, and IL-1beta and phosphorylation of ERK1/2...

Pimozide is a dopamine receptor antagonist (Kis = 2.4, 0.3, and 1.8 nM for D2, D3, and D4 receptors, respectively). It also binds to eight additional receptors (Kds = 25-3,100 nM for the human receptors) and inhibits the voltage-gated sodium channel Nav1.2 and the voltage-gated potassium channel Kv11.1 (IC50s = 42...

Heneicosapentaenoic Acid (HPA) is a fatty acid present in trace amounts in the green algae Bryopsis pennata Lamouroux and in fish oils. Its chemical composition is similar to eicosapentaenoic acid (EPA) except elongated with one carbon on the carboxyl end, placing the first double bond in the Delta6 position. HPA...

Cyproterone acetate (CPA) is an androgen receptor antagonist. It binds to human androgen receptors (Ki = 14 nM) and inhibits dihydrotestosterone-induced androgen receptor activation in CV-1 cells (IC50 = 26 nM). CPA (30 mg/kg) decreases ventral prostate weight in castrated immature rats. It also suppresses accessory...

RKI-1447 is an inhibitor of the Rho-associated kinases ROCK1 and 2 (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase. In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2...

CK-636 is an inhibitor of Arp2/3 complex action that binds the complex and inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC50s = 4, 32, and 24 µM, respectively). It is cell permeable, as it prevents actin polymerization and the formation of actin filament comet tails by...

Phenoxybenzamine is an antagonist of alpha-adrenergic receptors (alpha-ARs). It inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing alpha1-ARs (EC50s = 125.9-316.2 nM), as well as radioligand binding to alpha2A-, alpha2B-, and alpha2C-ARs in CHO cell membranes (Kis = 60, 10, and...

Smoothened (Smo) is a cell surface receptor that, with Patched, mediates sonic hedgehog (Shh) signaling to regulate gene expression through the Gli transcription factors. BMS 833923 is an orally bioavailable inhibitor of Smo. It blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell...

Jumonji AT-rich interactive domain 1 (JARID1) demethylases mediate the removal of methyl groups from trimethylated lysine 4 on histone 3 (H3K4me3). PBIT is a reversible, cell-permeable inhibitor of JARID1 family demethylases (IC50s = 6, 3, 4.9, and 28 µM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively). It...

Benztropine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 0.59 nM in rat brain membranes). It is selective for M1 receptors over the serotonin transporter (Ki = 5,150 nM), however, it also binds to the dopamine transporter and inhibits dopamine reuptake (Kis = 237 and 130 nM, respectively)....

CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively). It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM). At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines....