A potent Chk1 inhibitor
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SB 218078

Item No. 13335

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
135897-06-2
Molecular Formula
C24H15N3O3
Formula Weight
393.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 5 mg/ml
λmax
237, 278, 287, 318, 414 nm
SMILES
O=C(NC1=O)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5C7OC(CC7)N4C8=C3C=CC=C8
InChi Code
InChI=1S/C24H15N3O3/c28-23-19-17-11-5-1-3-7-13(11)26-15-9-10-16(30-15)27-14-8-4-2-6-12(14)18(22(27)21(17)26)20(19)24(29)25-23/h1-8,15-16H,9-10H2,(H,25,28,29)
InChi Key
OTPNDVKVEAIXTI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $156

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    Product Description

    SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC50 value of 15 nM.1 It less potently inhibits cdc2 and PKC (IC50s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 µM.1,2 SB 218078 releases G2 cell cycle arrest induced by γ-irradiation or the topoisomerase I inhibitor topotecan (Item No. 14129).1 In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jackson, J.R., Gilmartin, A., Imburgia, G., et al. An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage. Cancer Res. 60(3), 566-572 (2000).

    2. Tandon, M., Johnson, J., Li, Z., et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One 8(9), e75601 (2013).

    3. Kawabe, T. G2 checkpoint abrogators as anticancer drugs. Mol. Cancer Ther. 3(4), 513-519 (2004).