Search results for: 'research-area cell-cycle ksp'
Items 1-10 of 240
- AZD7762Catalog No. :A5919Checkpoint kinase inhibitor,ATP competitiveAZD7762 is a novel ATP competitive inhibitor of checkpoint kinases. Chk family checkpoint kinases include Chk1 and Chk2. They are activated in response to DNA damage and phosphorylate CDC25A, CDC25C protein phosphatases, which delay cell cycle progression. Therefore, Chk activation initiates cell cycle checkpoint, causes cell cycle arrest, and allows DNA repair.
- 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).
- MK-8776 (SCH-900776)Catalog No. :A8477Chk1 inhibitor,potent and selective
SCH 900776 is a potent and functionally selective inhibitor targeting cell cycle checkpoint kinase 1 (Chk1) (IC50 = 3 nM), Cdk2 (IC50 = 0.16 µM), and Chk2 (IC50 = 1.5 µM). Chk1 is an essential serine/threonine kinase which responds to DNA damage and stalls DNA replication, Chk1 is also essential for maintenance of replication fork viability during exposure to DNA antimetabolites. SCH 900776 is a weak inhibitor of CDK2.
- 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.
- 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.
- Rigosertib sodium saltCatalog No. :A1404Plk1 inhibitor
Rigosertib (ON-01910) is a potent, specific PLK1 inhibitor with IC50 value of 9nM. Rigosertib strongly inhibited the proliferation of cancer cell lines, with observed IC50 values in the nanomolar range for both HeLa (115 nM) and C33A (45 nM) cells. In contrast, rigosertib had a minimal effect on normal cell lines, BJ and Ect1/E6E7 (IC50 > 0.1 mM)
- Paclitaxel (Taxol)Catalog No. :A4393Antineoplastic agent
Paclitaxel is a novel antineoplastic agent, which was discovered in a screen of extracts of thousands of plants and natural products for antineoplastic activity by a National Cancer Institute program.
- MLN0905Catalog No. :A8680Potent PLK1 inhibitorMLN0905, a small-molecule PLK1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma.
- Vincristine sulfateCatalog No. :A1765Microtubule disrupter,antitumor agent
Vincristine is a naturally occurring alkaloid that potently inhibits the tubulin addition with the inhibition constant Ki value of 0.085 μM and exhibits an anti-proliferative activity against B16 melanoma cells with the half maximal inhibition concentration IC50 value of 0.45 M .
- AT7519 HydrochlorideCatalog No. :A3197Multi-CDK inhibitorIC50: AT7519 showed potent antiproliferative activity (40-940 nmol/L) in a panel of human tumor cell lines.