An inhibitor of Chk2 (IC50 = 200 nM in a cell-free kinase assay); selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk

NSC 109555 – 5 mg

Brand:
Cayman
CAS:
15427-93-7
Storage:
-20
UN-No:
Non-Hazardous - /

NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50 = 200 nM in a cell-free kinase assay).{24025} It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.{42938} NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.{42939}  

 

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Description

An inhibitor of Chk2 (IC50 = 200 nM in a cell-free kinase assay); selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK (IC50s = 210, 6,000, 7,400, and 7,100 nM, respectively); inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM); inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro; potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of ROS in MIA PaCa-2 cells at 1,250 nM

Formal name: 2,2′-[carbonylbis(imino-4,1-phenyleneethylidyne)]bis-hydrazinecarboximidamide, dimethanesulfonate

Synonyms:  DDUG|NCI C04808

Molecular weight: 600.7

CAS: 15427-93-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Cell Biology|Mitochondrial Biology

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