15427-93-7
Chemical Structure
NSC 109555
Synonym(s): DDUG; NCI C04808
- CAS No.: 15427-93-7
- Formula:C21H32N10O7S2
- Molecular Weight:600.67
IUPAC Name: (2E,2'E)-2,2'-(((carbonylbis(azanediyl))bis(4,1-phenylene))bis(ethan-1-yl-1-ylidene))bis(hydrazine-1-carboximidamide) dimethanesulfonate
InChIKey: HXDBGZUARNKHBV-XMDRLFCYSA-N
SMILES: C/C(C1=CC=C(C=C1)NC(NC2=CC=C(C=C2)/C(C)=N/NC(N)=N)=O)=N\NC(N)=N.O=S(C)(O)=O.O=S(C)(O)=O
Biological Activity: NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). 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.2 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.
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NSC 109555 | NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). 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.2 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. | |||||||||||||||||||||
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