usp1

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

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.

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

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.

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.

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.

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 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.

USP1-IN-9 (Compound 1m) is a reversible and non-competitive inhibitor of ubiquitin-specific protease (USP1) with an IC50 value of 8.8 nM. It is synthesized based on the structures of ML323 and KSQ-4279 as a pyrido[2,3-d]pyrimidin-7(8H)-one derivative. USP1-IN-9 exhibits excellent inhibition of USP1/UAF and demonstrates strong antiproliferative effects on breast cancer cells. When combined with the PARP inhibitor olaparib, USP1-IN-9 enhances the cytotoxic effect on MDA-MB-436/OP cells. USP1-IN-9 holds potential for research in the field of cancer.

USP1-IN-13 (compound 2) is a potent, orally active inhibitor of USP1 with an IC50 value of 0.00102 µM. It effectively suppresses cell colony formation.

USP1-IN-12 (compound 4) is a potent, orally active USP1 inhibitor with an IC50 value of 0.00366 µM. It is capable of inhibiting cell colony formation.

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-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-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]

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.

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-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-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.

USP10-IN-3 (compound D1) is a potent inhibitor of USP10, with an IC50 of 7.2 µM. It can suppress cell proliferation, induce apoptosis, and cause cell cycle arrest in the S phase.

USP10-IN-4 is a potent inhibitor of ubiquitin-specific protease 10 (USP10), with an IC50 of 10.87 μM and a Kd of 365 nM. It effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in liver cancer cells (apoptosis) and inhibits the initiation and progression of liver cancer. It is applicable in the study of hepatocellular carcinoma (HCC).

IU1-47 is an effective and specific USP14 inhibitor (IC50: 0.6 μM). IU1-47 causes tau elimination in cultured neurons. IU1-47 inhibits IsoT/USP5 (IC50: 20 μM).

Spautin-1 is an autophagy inhibitor that suppresses the deubiquitination activity of ubiquitin-specific peptidase USP10 and USP13. Spautin-1 inhibits UPR and exhibits preferential cytotoxicity in glucose-starved cancer cells.

PTP Inhibitor IV is an effective protein tyrosine phosphatase (PTP) inhibitor, which can selectively inhibit DUSP14 phosphatase activity (IC50.5.21μm). PTP Inhibitor IV inhibited SHP-2, PTP1B, PTp-ε, PTP Meg-2, PTP-σ, PTP-β and PTP-μ, IC50 were 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively. PTP Inhibitor IV affects cellular signaling by inhibiting PTP activity and may regulate specific pathways associated with PTP-mediated signaling events.

IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.