跳至主要内容

博文

A major introduction to Autophinib!

Autophinib(cas 1644443-47-9) is a potent autophagy inhibitor, which can inhibit autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34 with IC50s of 90, 40 and 19 nM, respectively.
最新博文

GW590735 CAS No. : 622402-22-6 is in stock now!

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.

E 3810 is in stock now!

First-in-class dual VEGFR/FGFR tyrosine kinase inhibitor; E-3810 potently and selectively inhibited VEGFR1, -2, and -3 and FGFR-1 and -2 kinases in the nanomolar range; a potent antiangiogenic small molecule with a favorable pharmacokinetic profile and broad spectrum antitumor activity

A major introduction to Cl316243!

CL 316243 disodium salt(151126-84-0) is a potent and highly selective β3-adrenoceptor agonist (EC50 = 3 nM); > 10000-fold selective over β1 and β2 receptors. Increases brown adipose tissue thermogenesis and metabolic rate, and decreases blood insulin and glucose levels following oral administration in vivo.

PIM447

PIM447(cas 1210608-43-7) is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase. PIM447 is cytotoxic for myeloma cells due to cell cycle disruption and induction of apoptosis mediated by a decrease in phospho-Bad (Ser112) and c-Myc levels and the inhibition of mTORC1 pathway. PIM447 also inhibits in vitro osteoclast formation and resorption, downregulates key molecules involved in these processes and partially disrupts the F-actin ring, while increasing osteoblast activity and mineralization.

Netarsudil Mesylate is in stock NOW!

Netarsudil Mesylate(cas 1422144-42-0) is a Rho kinase inhibitor with norepinephrine transport inhibitory activity that reduces production of aqueous humor. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.

A major introduction to BYL-719!

BYL719(cas 1217486-61-7) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, liitle or no effect on PI3Kβ/γ/δ. BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway.