SB-218078

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].

Product Specifications

CAS Number

[135897-06-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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

98.30

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C24H15N3O3

Molecular Weight

393.39

Precautions

H302, H315, H319, H335

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.