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CHK1 protein kinase inhibitor SB 218078, 1 mg  

CHK1 protein kinase inhibitor SB 218078, 1 mg

9,10,11,12-Tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'- kl]pyrrolo[3,4 - i][1,6]benzodiazocine-1,3(2H)-dione

Synonyms: SB218078, SB-218078
ATP-competitive inhibitor of Chk1

More details

PKI-SB218-001

Availability: within 3 days

215,00 €

Background: SB 218078 is a potent ATP-competitive inhibitor of Chk1, a serine-threonine kinase that is critical for G2/M arrest in response to DNA damage. The structure of SB 218078 is related to staurosporine, an unselective kinase inhibitor. SB 218078 inhibits Chk1 activity in vitro with an IC50 of 15 nM whereas it displays less inhibitory activity against CDK1/CycB and PKC (IC50 = 250 nM and 1000 nM). In cellular assays SB 218078 was able to abrogate G2 arrest in response to DNA damage and enhance the cytotoxicity of DNA-damaging drugs.

Chemical formula: C24H15N3O3
Molecular weight: 393.4 g/mol
Purity: >98% (TLC, HPLC)
Solubility: soluble to 100 mM DMSO
CAS Number: 135897-06-2

Product specific literature references:

Jackson JR, Gilmartin A, Imburgia C, Winkler JD, Marshall LA, Roshak A. (2000) "An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage." Cancer Res. 60(3):566-72.

Kawabe T. (2004) "G2 checkpoint abrogators as anticancer drugs." Mol Cancer Ther. 3(4):513-9.

Zhao B, Bower MJ, McDevitt PJ, Zhao H, Davis ST, Johanson KO, Green SM, Concha NO, Zhou BB. (2002) "Structural basis for Chk1 inhibition by UCN-01." J Biol Chem. 277(48):46609-15.

Wang XM, Li J, Feng XC, Wang Q, Guan DY, Shen ZH. (2008) "Involvement of the role of Chk1 in lithium-induced G2/M phase cell cycle arrest in hepatocellular carcinoma cells." Cell Biochem. 104(4):1181-91.

Product Citations:

Albiges L, Goubar A, Scott V, Vicier C, Lefèbvre C, Alsafadi S, Commo F, Saghatchian M, Lazar V, Dessen P, Delaloge S, André F, Quidville V (2014) "Chk1 as a new therapeutic target in triple-negative breast cancer." Breast. 23(3):250-8.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.