10 products were found matching "Cay16851"!

Evodiamine is a natural indole alkaloid found in the fruits of Wu Zhu Yu, a plant used in traditional Chinese medicine. Studies involving evodiamine have demonstrated beneficial effects in cancer, obesity, inflammation, and many other conditions. It can act as an aryl hydrocarbon antagonist (Ki = 28 nM), activator...

Bavachin is a flavonoid first isolated from seeds of P. corylifolia. It is a phytoestrogen that activates the estrogen receptors ERalpha and ERbeta (EC50s = 320 and 680 nM, respectively). Through this action, bavachin stimulates osteoblast proliferation and differentiation and prevents bone loss following...

alpha-Bungarotoxin is a snake venom-derived toxin that irreversibly binds nicotinic acetylcholine receptors (Ki = ~2.5 µM in rat) present in skeletal muscle, blocking action of acetylcholine at the postsynaptic membrane and leading to paralysis. It has been widely used to characterize activity at the neuromuscular...

Rp-Cyclic AMPS (Rp-cAMPS) is a non-hydrolyzable phosphorothioate analog of cAMP. It is a competitive inhibitor of cAMP-dependent protein kinases I and II (IC50s = 12.5 and 4.5 µM, respectively). Rp-cAMPS is not hydrolyzed by bovine heart cAMP phosphodiesterase but can be hydrolyzed by yeast phosphodiesterase. It is...

Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis. CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It...

TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively). It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases. TAK-632 shows significant antiproliferative activity against mutated B-Raf or...

15(R)-17-phenyl trinor Prostaglandin F2alpha isopropyl ester (15(R)-17-phenyl trinor PGF2alpha isopropyl ester) is the latanoprost-related isomer containing both a double bond at 13,14 and an inverted (beta) hydroxyl group at C-15. Similar to 15(S)-latanoprost, 15(R)-17-phenyl trinor PGF2alpha isopropyl ester is a...

1-thio-beta-D-Glucose is an analog of beta-D-glucose in which sulfur replaces the hydroxyl group at the one position. The thiol group allows diverse chemical reactions, including the thiol-Michael addition reaction and polymerization. 1-thio-beta-D-Glucose can be labeled with technetium-99m for analytical and...

A number of 17-phenyl trinor prostaglandin F2alpha (17-phenyl trinor PGF2alpha) derivatives have been approved for the treatment of glaucoma. Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side...

AZ 505 is an inhibitor of the lysine N-methyltransferase SMYD2 (IC50 = 0.12 µM). It is selective for SMYD2 over SMYD3, DOT1L, EZH2, GLP, G9A, and SET7/9 (IC50s = >83.3 µM). AZ 505 (10 mg/kg) delays cyst growth in early- and late-stage Pdk1 conditional knockout mouse models of polycystic kidney disease.Formal Name:...