9 products were found matching "Cay13644-%25"!

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin) and regulate different pathways. PP242 is an inhibitor of the active site of mTOR kinase in...

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM). AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis...

Alfuzosin is a post-synaptic alpha1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH). It displays high-affinity with non-selectivity for the three known human alpha1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for alpha1A, alpha1B, and...

GW 856553X is a dual inhibitor of p38alpha and p38beta MAPK (Kis = 0.0079 and 0.025 µM, respectively, in cell-free assays). It is selective for p38alpha and p38beta MAPK over p38gamma and p38delta MAPK when used at a concentration of 10 µM. GW 856553X inhibits LPS-induced TNF-alpha production in isolated rat and...

Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (Kd1 = 3 nM, Kd2 = 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically...

WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of phosphatidylinositol 3-kinase alpha (IC50 = 1,026 nM) and other kinases. WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and...

Icariin is a prenylated flavonoid that has been found in E. pubescens and has diverse biological activities. It induces the differentiation of ES-D3 embryonic stem cells into cardiomyocytes when used at concentrations of 10 and 100 µM. Icariin (10 µM) increases the mRNA expression of RUNX family transcription factor...

Anecortave acetate is a sterol lipid. It inhibits VEGF-induced increases in vascular generation, number, and length in isolated rat retinas when used at a concentration of 1 µM. Sub-tenon administration of anecortave acetate (7.5% w/v) prevents and reduces increases in intraocular pressure induced by prednisolone...

LEE011 is a cyclin-dependent kinase 4 (Cdk4) and Cdk6 inhibitor (IC50s = 0.53 and 2.3 nM, respectively). It is selective for Cdk4/6 over Cdk1, Cdk2, Cdk5, Cdk7, and Cdk9 (IC50s = >1,400, >2,500, >2,000, >2,000, and 190 nM, respectively). LEE011 reduces the proliferation of MCF-7 and T47D breast cancer cells (IC50s =...