An inhibitor of the ERCC-1-XPF protein-protein interaction
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HM03

Item No. 40908

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(6-chloro-2-methoxy-9-acridinyl)amino]-2-[(4-methyl-1-piperazinyl)methyl]-phenol
CAS Number
500565-15-1
Molecular Formula
C26H27ClN4O2
Formula Weight
463.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
ClC(C=CC1=C2NC3=CC=C(O)C(CN4CCN(CC4)C)=C3)=CC1=NC5=C2C=C(OC)C=C5
InChi Code
InChI=1S/C26H27ClN4O2/c1-30-9-11-31(12-10-30)16-17-13-19(4-8-25(17)32)28-26-21-6-3-18(27)14-24(21)29-23-7-5-20(33-2)15-22(23)26/h3-8,13-15,32H,9-12,16H2,1-2H3,(H,28,29)
InChi Key
SUSDGTMJKOGWSZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $38

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    10 mg

    $72

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    25 mg

    $169

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    50 mg

    $281

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    Cayman Chemical
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    Product Description

    HM03 is an inhibitor of the protein-protein interaction between the DNA excision repair protein ERCC-1 and the DNA repair endonuclease XPF (IC50 = 1.86 µM).1 It is also an inhibitor of D-alanine-D-alanine ligase B (DdlB; Ki = 218 µM for the E. coli enzyme).2 HM03 is active against E. coli and S. aureus (MICs = 64 and 32 µg/ml, respectively). It potentiates cytotoxicity induced by cisplatin (Item No. 13119) in A549 lung and HCT116 colon cancer cells when used at a concentration of 100 µM.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Elmenoufy, A.H., Gentile, F., Jay, D., et al. Targeting DNA repair in tumor cells via inhibition of ERCC1-XPF. J. Med. Chem. 62(17), 7684-7696 (2019).

    2. Kovac, A., Konc, J., Vehar, B., et al. Discovery of new inhibitors of D-alanine:D-alanine ligase by structure-based virtual screening. J. Med. Chem. 51(23), 7442-7448 (2008).

    3. Jordheim, L.P., Barakat, K.H., Heinrich-Balard, L., et al. Small molecule inhibitors of ERCC1-XPF protein-protein interaction synergize alkylating agents in cancer cells. Mol. Pharmacol. 84(1), 12-24 (2013).