Search results for: 'research-area stem-cell hippo-signaling'
- 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.
- R547Catalog No. :A8642CDK1/2/4 inhibitor,ATP-competitive
R547 is a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases with a Ki of median 2 nM for CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1((Ki=0.001,0.003,and 0.001 μM for CDK1,CDK2, and CDK4,respectively).
- BS-181 HClCatalog No. :A5700CDK7 inhibitor,highly selective
Normal progression through the cell cycle requires the sequential action of cyclin-dependent kinases CDK1, CDK2, CDK4, and CDK6. Direct or indirect deregulation of CDK activity is a feature of almost all cancers and has led to the development of CDK inhibitors as anticancer agents.
- AT7519 HydrochlorideCatalog No. :A3197Multi-CDK inhibitorIC50: AT7519 showed potent antiproliferative activity (40-940 nmol/L) in a panel of human tumor cell lines.
- LEE011Catalog No. :A8641CDK4/6 inhibitorLEE011 (NVP-LEE011) is a highly specific inhibitor of CDK4/CDK6 and functions via decreasing in phosphorylated RB and FOXM1.
- Dinaciclib (SCH727965)Catalog No. :A8412Potent CDK inhibitor
Dinaciclib is a potent cyclin-dependent kinase (CDK) inhibitor with IC50s for CDK2, CDK5, CDK1 and CDK9 at 1 nM, 1 nM, 3 nM, and 4 nM, respectively. It is in phase I or II clinical trials for various cancers.
- BMS265246Catalog No. :A8385CDK1/2 inhibitor,potent and selectiveBMS265246 is a potent and selective Cdk1/Cdk2 inhibitor for Cdk1/cyclin-B (IC50 = 6 nM) and Cdk2/cyclin-E (IC50 = 9 nM).
- 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.
- Palbociclib (PD0332991) IsethionateCatalog No. :A8335CDK4/6 inhibitor,highly selective
Description:IC50: Palbociclib is an orally active, potent and highly selective inhibitor of CDK4 and CDK6, with IC50 values for CDK4/cyclinD1, CDK4/cyclinD3 and CDK6/cyclinD2 of 11, 9 and 15 nmol/l, respectively.