A TRIP13 inhibitor
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DCZ0415

Item No. 42513

Technical Information
Formal Name
4,4a,5,5a,6,6a-hexahydro-2-[4-(4-pyridinylmethyl)phenyl]-4,6-ethenocycloprop[f]isoindole-1,3(2H,3aH)-dione
CAS Number
2242470-43-3
Molecular Formula
C23H20N2O2
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C1N(C(C2C3C=CC(C4CC34)C12)=O)C5=CC=C(CC6=CC=NC=C6)C=C5
InChi Code
InChI=1S/C23H20N2O2/c26-22-20-16-5-6-17(19-12-18(16)19)21(20)23(27)25(22)15-3-1-13(2-4-15)11-14-7-9-24-10-8-14/h1-10,16-21H,11-12H2
InChi Key
LOXMLWHUIONWMI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    DCZ0415 is an inhibitor of thyroid hormone receptor interactor 13 (TRIP13).1 It binds to TRIP13 (Kd = 2.42 µM) and reduces non-homologous end joining (NHEJ) repair of DNA in a reporter assay. DCZ0415 (10 and 20 µM) impairs DNA repair in ARP-1 and NCI H929 multiple myeloma cells. It reduces the growth of a variety of multiple myeloma cells, including RPMI-8226, ARP-1, and ARK cells (IC50s = 7.4, 5.12, and 3.25 µM, respectively) and induces apoptosis in ARP-1 cells. DCZ0415 (50 mg/kg per day) induces intratumoral apoptosis and impairs intratumoral DNA repair, reduces tumor volume, and increases survival in an NCI H929 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, Y., Huang, J., Li, B., et al. A small-molecule inhibitor targeting TRIP13 suppresses multiple myeloma progression. Cancer Res. 80(3), 536-548 (2020).