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SB-218078

Product Specifications

UNSPSC Description

SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest[1][2][3].

Target Antigen

Apoptosis; CDK; Checkpoint Kinase (Chk); PKC

Type

Reference compound

Related Pathways

Apoptosis;Cell Cycle/DNA Damage;Epigenetics;TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sb-218078.html

Purity

98.3

Solubility

10 mM in DMSO

Smiles

O=C1NC(C(C2=C3N(C4CCC5O4)C6=CC=CC=C62)=C1C7=C3N5C8=CC=CC=C78)=O

Molecular Weight

393.39

References & Citations

[1]Jackson JR, et al. An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 2000 Feb 1;60(3):566-72.|[2]Murga M, et al. Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors. Nat Struct Mol Biol. 2011 Nov 27;18(12):1331-1335.|[3]Preet R, et al. Chk1 inhibitor synergizes quinacrine mediated apoptosis in breast cancer cells by compromising the base excision repair cascade. Biochem Pharmacol. 2016 Apr 1;105:23-33.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-107407/SB-218078-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-107407/SB-218078-SDS-MedChemExpress.pdf

Clinical Information

No Development Reported

CAS Number

135897-06-2

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