A Chk2 inhibitor (IC50 = 13.5 nM); selective for Chk2 over Chk1 (IC50 = 220.4 nM); inhibits Chk2 autophosphorylation at Ser516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 at 0.1-30 µM; enhances survival of 184B5

Chk2 Inhibitor – 500 µg

Brand:
Cayman
CAS:
724708-21-8
Storage:
-20
UN-No:
Non-Hazardous - /

Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2; IC50 = 13.5 nM).{48513} It is selective for Chk2 over Chk1 (IC50 = 220.4 nM). It inhibits Chk2 autophosphorylation at the serine in position 516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 when used at concentrations ranging from 0.1 to 30 µM. Chk2 inhibitor enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation and inhibits cell cycle arrest at the G2 stage induced by ionizing radiation in 184B5 cells. It also inhibits the production of IL-2 in Jurkat cells stimulated by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) and the production of TNF-α in LPS-stimulated THP-1 cells (IC50s = 3.5 and 8.2 µM, respectively).{48514} Chk2 inhibitor also inhibits the growth of CEM leukemia T cells (GI50 = 1.73 µM).  

 

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Description

A Chk2 inhibitor (IC50 = 13.5 nM); selective for Chk2 over Chk1 (IC50 = 220.4 nM); inhibits Chk2 autophosphorylation at Ser516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 at 0.1-30 µM; enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation; inhibits PMA-induced production of IL-2 in Jurkat cells and LPS-induced TNF-α production in THP-1 cells (IC50s = 3.5 and 8.2 µM, respectively); inhibits the growth of CEM leukemia T cells (GI50 = 1.73 µM)

Formal name: (5Z)-5-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-3,4,5,10-tetrahydro-azepino[3,4-b]indol-1(2H)-one

Synonyms:  SC-203885

Molecular weight: 295.3

CAS: 724708-21-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Innate Immunity

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