USP1-IN-9

• Description:

  USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7 (8H) -one derivative based on the disclosed structure of ML323 (HY-17543) and KSQ-4279 (HY-145471) . USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib (HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer[1].

• UNSPSC:

  12352005

• Target:

  Deubiquitinase

• Type:

  Reference compound

• Related Pathways:

  Cell Cycle/DNA Damage

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/usp1-in-9.html

• Smiles:

  O=C1C=CC2=CN=C(C3=C(C4CC4)N=CN=C3OC)N=C2N1CC5=CC=C(C6=NC(C(F)(F)F)=CN6C(C)C)C=C5

• Molecular Formula:

  C29H26F3N7O2

• Molecular Weight:

  561.56

• References & Citations:

  [1][1] Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7 (8H) -one derivatives as potent USP1 inhibitors[j]. Eur J Med Chem. 2024 Jun 14;275:116568.https://pubmed.ncbi.nlm.nih.gov/38889606/|[2][1] Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7 (8H) -one derivatives as potent USP1 inhibitors[j]. Eur J Med Chem. 2024 Jun 14;275:116568.https://pubmed.ncbi.nlm.nih.gov/38889606/|[3][1] Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7 (8H) -one derivatives as potent USP1 inhibitors[J]. Eur J Med Chem. 2024 Jun 14;275:116568.https://pubmed.ncbi.nlm.nih.gov/38889606/|[4]Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7 (8H) -one derivatives as potent USP1 inhibitors[J]. Eur J Med Chem. 2024 Jun 14;275:116568.|[5]Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7 (8H) -one derivatives as potent USP1 inhibitors[J]. Eur J Med Chem. 2024 Jun 14;275:116568.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [2925548-22-5]