CHK2 INHIBITOR II
CHK2 INHIBITOR II Basic information
- Product Name:
- CHK2 INHIBITOR II
- Synonyms:
-
- 2-(4-(4-CHLOROPHENOXY)PHENYL)-1H-BENZO[D]IMIDAZOLE-5-CARBOXAMIDE, >98%
- BML-277, >98%
- BML-277 (C 3742)
- CS-1761
- BML-277,CHK2 INHIBITOR II
- CHK2 INHIBITOR II; C 3742; BML277; BML 277
- Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem
- InSolution Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem
- CAS:
- 516480-79-8
- MF:
- C20H14ClN3O2
- MW:
- 363.8
- Product Categories:
-
- Inhibitors
- API
- Mol File:
- 516480-79-8.mol
CHK2 INHIBITOR II Chemical Properties
- Boiling point:
- 637.1±63.0 °C(Predicted)
- Density
- 1.390±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: 18 mg/mL
- form
- solid
- pka
- 10.40±0.10(Predicted)
- color
- tan
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
CHK2 INHIBITOR II Usage And Synthesis
Description
Chk2 inhibitor II is a selective, ATP-competitive inhibitor of the DNA damage control kinase, checkpoint kinase 2 (IC50 = 15 nM). It has been shown to prevent apoptosis in human T-cells exposed to ionizing radiation (EC50 = 3-7.6 μM). This compound has been used to target the role of Chk2 in cellular signaling in response to DNA damage.
Uses
Chk2 Inhibitor II is a selective APT-competitive inhibitors of the DNA damage response signaling enzyme checkpoint kinase 2 (CHK2).
Biochem/physiol Actions
Chk2 Inhibitor II is a checkpoint kinase 2 inhibitor, which controls the p53 response to DNA breaks induced by radiation, leading to apoptosis. Protection of T-cells from apoptosis implies use as an adjuvant for radiation therapy in cancer. IC50 = 15 nM; Ki = 37 nM. Chk2 Inhibitor II shows 1000-fold greater selectivity for the Chk2 serine/threonine kinase than for the Cdk1/B and CK1 kinases (for which IC50 = 12 μM and 17 μM, respectively). Chk2 Inhibitor II weakly inhibits a panel of 31 other kinases (<25% inhibition at a concentration of 10 μM and prevents apoptosis of human CD4+ and CD8+ T-cells subjected to ionizing radiation (EC50 = 3 μM and 7.6 μM, respectively).
References
1) Arienti et al. (2005), Checkpoint kinases inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles; J. Med. Chem., 48 1873 2) Pereg et al. (2006), Differential roles of ATM- and Chk2-mediated phosphorylations of Hdmx in response to DNA damage; Mol. Cell. Biol., 26 6819
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