A selective Chk1 inhibitor
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CHIR124

Item No. 16553

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-2(1H)-quinolinone
CAS Number
405168-58-3
Molecular Formula
C23H22ClN5O
Formula Weight
419.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 10 mg/ml
λmax
241, 288, 375 nm
SMILES
O=C(C(C1=NC2=C(C=CC=C2)N1)=C3N[C@@H]4CN5CCC4CC5)NC6=C3C=C(Cl)C=C6
InChi Code
InChI=1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1
InChi Key
MOVBBVMDHIRCTG-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. CHIR124 is a cell-permeable, quinolone-based inhibitor of Chk1 (IC50 = 0.3 nM in vitro).1 It demonstrates high selectivity for Chk1 by displaying inhibitory values 2,000-fold higher against Chk2 (IC50 = 0.7 µM).1 In synergy with topoisomerase I poisons or ionizing radiation, CHIR124 can inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, potentiating tumor apoptosis.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tse, A.N., Rendahl, K.G., Sheikh, T., et al. CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clin. Cancer Res. 13(2 Pt 1), 591-602 (2007).

    2. Tao, Y., Leteur, C., Yang, C., et al. Radiosensitization by Chir-124, a selective CHK1 inhibitor: Effects of p53 and cell cycle checkpoints. Cell Cycle 8(8), 1196-1205 (2009).