2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Deubiquitinase
  5. USP1 Isoform

USP1

Deubiquitinase USP1 regulates DNA damage response by removing ubiquitin from FANCD2, FANCI, and PCNA, thereby controlling Fanconi anemia signaling and translesion DNA synthesis[1][2]. Mechanistically, USP1 functions with UAF1, which activates USP1 and supports FANCD2 and PCNA deubiquitination in DNA repair contexts[2][3]. In homologous recombination models, USP1/UAF1 promotes double-strand break repair and suppresses nonhomologous end joining[3]. DNA and RAD51AP1 further support efficient FANCD2 deubiquitination by the USP1-UAF1 complex[4]. Compared with broader USP family activity, USP1 shows substrate specificity through its conserved N-terminus, which drives FANCD2 deubiquitination but is not required for PCNA or FANCI deubiquitination[5]. In cancer models, selective USP1/UAF1 inhibitors such as ML323, pimozide, and GW7647 enhance cisplatin responses in non-small cell lung cancer, osteosarcoma, and cisplatin-resistant NSCLC cells[2][6]. In HPV-negative HNSCC models, reduced SERPINB3 decreases USP1-mediated FANCD2-FANCI deubiquitination and increases cisplatin-induced apoptosis[7]. Therefore, USP1 inhibitors serve as practical probes for studying DNA repair, Fanconi anemia pathway regulation, and chemotherapy response mechanisms[2][6].

USP1 Related Products (11):

Cat. No. Product Name Effect Purity
  • HY-145471
    KSQ-4279
    		Inhibitor 99.96%
    KSQ-4279 (USP1-IN-1) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 is promising for research of cancers.
  • HY-145471A
    KSQ-4279 gentisate
    		Inhibitor 99.75%
    KSQ-4279 (gentisate) (Compound Formula I) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 (gentisate) is promising for research of cancers.
  • HY-148099
    USP1-IN-2
    		Inhibitor 99.76%
    USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM. USP1-IN-2 can be used for the study of cancers such as osteosarcoma.
  • HY-183581
    USP1-IN-18
    		Inhibitor
    USP1-IN-18 is an orally active USP1 inhibitor with a human IC50 of 17.0 nM. USP1-IN-18 inhibits USP1-UAF1 deubiquitinase activity and drives ubiquitinated PCNA accumulation. USP1-IN-18 induces DNA damage, replication stress, and G2-M phase cell cycle arrest. USP1-IN-18 can be used for the research of triple-negative breast cancer.
  • HY-176704
    USP1-IN-13
    		Inhibitor
    USP1-IN-13 (Compound 2) is a potent and orally active USP1 inhibitor with an IC50 value of 1.02 nM. USP1-IN-13 can be used for the study of breast cancer.
  • HY-181702
    USP1-IN-16
    		Inhibitor
    USP1-IN-16 is a USP1 inhibitor with an USP1-UAF1 IC50 value of 0.002 μM. USP1-IN-16 can be used in the research of USP1-related malignancies.
  • HY-180216
    USP1-IN-15
    		Inhibitor
    USP1-IN-15 is an orally active and selective USP1 inhibitor with an IC50 of 12.3 nM. USP1-IN-15 has a high specificity for USP1 with negligible inhibition against all off-target DUBs. USP1-IN-15 suppresses colony formation, induces S-phase arrest, and stabilizes ubiquitinated PCNA. USP1-IN-15 also shows synergistic antiproliferative activity. USP1-IN-15 achieves significant tumor growth inhibition in vivo. USP1-IN-15 can be used for BRCA-mutated breast cancer.
  • HY-161878
    USP1-IN-10
    		Inhibitor
    USP1-IN-10 (compound 2) is a potent tricyclic USP1 inhibitor with an IC50 of 7.6 nM. USP1-IN-10 inhibits MDA-MB-436 viability (IC50=21.58 nM). USP1-IN-10 has the potential for cancers research.
  • HY-176703
    USP1-IN-12
    		Inhibitor
    USP1-IN-12 (compound 4) is a potent and orally activeUSP1 inhibitor with an IC50 value of 0.00366 µM. USP1-IN-12 inhibits cell clone formation.
  • HY-179292
    USP1-IN-14
    		Inhibitor
    USP1-IN-14 (compound 27) is a ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of 0.001 µM. USP1-IN-14 can be used for USP1-related cancers, autoimmune and inflammatory disorders research.
  • HY-153731
    USP1-IN-4
    		Inhibitor
    USP1-IN-4 (compound 10) is an effective USP1 inhibitor with an IC50 value of 2.44 nM. USP1-IN-4 has anticancer activity and synergistic activity with various anticancer drugs.