USP1 Inhibitor

KSQ-4279 (USP1-IN-1) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 is promising for research of cancers.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.