Search results for: 'research-area gpcr-g-protein'
- PHA-848125Catalog No. :A8501CDK inhibitor,potent and ATP-competitivePHA-848125 is a potent, ATP-competitive Cdk2/cyclin A inhibitor (IC50 = 45 nM). PHA-848125 also inhibits additional cdk proteins, but to significantly lesser extent; the activities of Cdk7/cyclin H (IC50 = 0.15 µM), Cdk4/cyclin D1 (IC50 = .0.16 µM), Cdk5/p35 (IC50 = 0.265 µM), as well as Cdk2/cyclin E (IC50 = 0.363 µM) and Cdk1/cyclin B (IC50 = 0.398 µM). Trk A (NTRK1) is also inhibited by PHA-848125 with similar potency to the Cdk’s. PHA-848125 also impairs phosphorylation of the retinoblastoma (Rb) protein at Cdk2 and Cdk4 specific sites, reduces retinoblastoma protein and cyclin A levels, and increases p21(Cip1), p27(Kip1) and p53 expression.
- 1-NM-PP1Catalog No. :B1299Pp60c-src inhibitor1-NM-PP1 is a C3-modified analog of cell-permeable PP1, acts as a potent and selective inhibitor of protein kinase families .
- A-674563Catalog No. :A8616Akt1/PKA/CDK2 inhibitor,potent and selectiveA-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM.
- AZD-5438Catalog No. :A8326Potent CDK1/2/9 inhibitor
AZD5438 is a potent small molecule inhibitor of cyclin-dependent kinase (CDK) 1, 2 and 9 with half maximal inhibitory concentration IC50 of 16 nmol/L, 6 nmol/L and 20 nmol/L respectively. AZD5438 has also been found to potently inhibit the human cyclin E/CDK2 complex, the cyclin B1/CDK1 complex and the cyclin A/CDK2 complex with IC50 of 0.006 μM, 0.016 μM and 0.045 μM respectively. In previous studies, AZD5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with IC50 ranging from 0.2 μmol/L to 1.7 μmol/L, in which the phosphorylation of a few proteins, including CDK substrates pRb, nucleolin, protein phosphatase 1a and RNA polymerase II COOH-terminal domain, and cell cycling at G2-M, S and G1 phases were inhibited.