usp1

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.

USP1-IN-2 is a potent USP1 inhibitor with potential anti-tumor activity for the study of cancer.

USP1-IN-7 (Compound 3), a potent inhibitor of ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, exhibits an inhibition concentration (IC 50) of ≤50 nM. It also effectively inhibits the proliferation of MDA-MB-436 cells at similar concentrations [1].

USP1-IN-3 is a selective inhibitor of USP1, effectively inhibiting USP1-UAF1 with an IC50 of less than 30 nM. USP1-IN-3 is utilized for cancer research.

USP1-IN-6 (Compound 11) functions as a potent USP1 inhibitor, exhibiting an IC50 value of less than 50 nM. Additionally, it demonstrates inhibitory activity against MDA-MB-436 cells with a comparable IC50. [1]

USP1-IN-5 (compound 10) is a potent inhibitor of USP1, with an IC50 of less than 50 nM, and of MDA-MB-436 cells, exhibiting an IC50 of less than 50 nM [1].

USP1-IN-10 (compound 2) is an effective tricyclic USP1 inhibitor with an IC50 of 7.6 nM. It inhibits the viability of MDA-MB-436 cells with an IC50 of 21.58 nM, demonstrating potential for use in cancer research.

USP1-IN-4 (compound 10) serves as a potent inhibitor of USP1, exhibiting an IC 50 of 2.44 nM. It demonstrates anticancer properties and operates synergistically with various anticancer drugs [1].

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It promotes the activation of the DDR (DNA damage repair) pathway, inducing cell cycle arrest and apoptosis, thereby inhibiting cell viability. USP1-IN-11 increases the sensitivity of cells resistant to Olaparib and shows synergistic effects with Andrographolide in cancer cells with normal BRCA function. In the MDA-MB-436 xenograft model, USP1-IN-11 exhibits a significant dose-dependent antitumor effect.

USP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM) with high antiproliferative activity against non-small cell lung cancer and leukemia cells. As an interacting protein of cGAS, USP15 promotes cGAS to recognize DNA and activate downstream signaling pathways.

SJB3-019A is a potent, potent and novel ubiquitin-specific protease 1 (USP1) inhibitor, which promotes ID1 degradation and cytotoxicity in K562 cells 5 times more than SJB2-043, with IC50 of 0.0781 μM. SJB3-019A inhibits cell proliferation and causes cell apoptosis.

ML323 is a reversible and effective USP1-UAF1 inhibitor in a Ub-Rho assay (IC50: 76 nM) and in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) (IC50: 174 nM 820 nM)and monoubiquitinated PCNA (Ub-PCNA) (IC50: 820 nM) as substrates, respectively.

C527 is a potent pan DUB enzyme inhibitor with a high affinity for the USP1 UAF1 complex (IC50=0.88 μM).

SJB2-043, an inhibitor of USP1-UAF1, has an IC50 of 544 nM.

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.

I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.

KSQ-4279 (gentisate) (Compound Formula I) serves as an effective inhibitor of USP1 and a selective inhibitor of PARP1. This compound shows promise for use in cancer research.