Chk2 Inhibitor II hydrate

• Catalog No.: C3742
• CAS Number: 516480-79-8(anhydrous)
• M. F.: C20H14ClN3O2
• M. W.: 363.79706
• Purity: ≥98% (HPLC)

SYNONYMS

• IUPAC name: 2-[4-(4-chlorophenoxy)phenyl]-1H-1,3-benzodiazole-5-carboxamide
• IUPAC Traditional name: 2-[4-(4-chlorophenoxy)phenyl]-1H-1,3-benzodiazole-5-carboxamide
• Synonyms: 2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide hydrate

DATABASE IDS

• MDL Number: MFCD08276917
• PubChem SID: 24724438
• CAS Number: 516480-79-8(anhydrous)

PROPERTIES

• Empirical Formula (Hill Notation): C20H14ClN3O2 · xH2O
• Purity: ≥98% (HPLC)
• Gene Information: human ... CHEK2(11200)
• Apperance: off-white to tan solid
• Solubility: DMSO: >10 mg/mL
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

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).

Description (简体中文)

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).