USP1-IN-9

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].

Product Specifications

CAS Number

[2925548-22-5]

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.