SB-218078

• 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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Chk1; PKC

• CAS Number:

  [135897-06-2]