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Medchemexpress LLC I-138 | 2098211-50-6 | C26H23F3N6O | 1 MG
SDP

Supplier:  Medchemexpress LLC HY1533651MG

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I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells.

  • Orally active and reversible inhibitor of USP1-UAF1.
  • Potent inhibitory activity against USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM).
  • Induces monoubiquitination of FANCD2 and PCNA in cells.
  • Eliminates USP1 autocleavage in cells.
  • Demonstrates modest antitumor activity in mice bearing MDA-MB-436 tumors.
  • Shows enhanced inhibition of BRCA1/2 mutant tumors in vivo when combined with the PARP inhibitor Niraparib.

Catalog No. 50-003-72822


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