DUB

DUB-IN-1, with an IC50 value of 0.24 for USP8, is an active inhibitor of ubiquitin-specific protease (USPs).

Dub-in-2, with an IC50 value of 0.28 for USP8, is an effective deubiquitinase inhibitor.

DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor with an IC50 of 0.56 μM for USP8.

GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy.

VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 ranging from 4.2 μM to 8.6 μM, and exhibits potent inhibition of USP14.

DUB-IN-7 (compound 43), a deubiquitinating enzyme (DUB) inhibitor, has utility in researching diseases driven by aberrant JAK2 activity, including leukemia [1].

DUB-IN-8 (Compound 8q) serves as an inhibitor of Chlamydia deubiquitinase 1 (DUB1) with an IC50 of 7.7 μM. It exhibits antibacterial properties by inhibiting Chlamydia inclusions, with an IIC50 [the concentration to induce 50% inclusion inhibition] of 8.5 μg/mL.

ChlaDUB1-IN-2 (Compound 27a) serves as an inhibitor of the deubiquitinating enzyme ChlaDUB1 from Chlamydia trachomatis, with an IC50 of 0.97 μM. It also inhibits the formation of Chlamydia trachomatis inclusions, exhibiting an IIC50 of 25.6 μg mL.

Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco[1].

ChlaDUB1-IN-1 (Compound 8) is an inhibitor of the Chlamydia deubiquitinase enzyme 1 (ChlaDUB1) and serves as a potential agent in antimicrobial research.

Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.

Seco-DUBA is an anticancer DNA alkylating agent and prodrug of DUBA, which can be used as a cytotoxic antibody-drug conjugate (ADC). It has an IC50 of 18 nM against KB and 430 pM against SK-OV-3, and can be converted into DUBA with higher stability and activity in vivo.

Seco-DUBA hydrochloride, a toxin used in the antibody-drug conjugate (ADC) SYD985.

Sudubrilimab (HS636), an Ig G1-kappa monoclonal antibody targeting PDL1, is engineered with a TGF-β1 receptor II ectodomain (TGFBR2-ECD) fused to its C-terminus. This design enables Sudubrilimab to simultaneously inhibit the PD-1/PD-L1 pathway and TGF-β bioactivity within the immunosuppressive tumor microenvironment [1].

Meliadubin B, a natural triterpenoid, effectively inhibits inflammatory responses by suppressing superoxide anion generation in human neutrophils (EC 50 of 5.54 μM) as well as inducible nitric oxide synthase activity. Additionally, it demonstrates significant antifungal properties against the rice pathogen Magnaporthe oryzae, with an IC 50 of 182.50 μM.

Desmethyl Vc-seco-DUBA, a compound comprising a cleavable ADC linker (Desmethyl Vc-seco) and a DNA alkylating agent (DUBA), is utilized in the synthesis of antibody-drug conjugates (ADCs) [1].

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).

IMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.IMP-1710 has antifibrotic activity. [1]

6RK73 is a covalent, irreversible, and specific UCHL1 inhibitor (IC50: 0.23 µM) with almost no inhibition of UCHL3 (IC50: 236 µM).

Capzimin is a selective inhibitor of proteasome isopeptidase Rpn11.

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.

USP30 inhibitor 11 (USP30-IN-11) is a selective USP30 inhibitor (IC50: 0.01 µΜ) that inhibits SVA and can be used in studies of cancer, mitochondrial dysfunction and Parkinson's.

Vialinin A (Terrestrin A), a p-terphenyl compound, exhibits antioxidant properties and acts as a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Its efficacy in autoimmune diseases and cancer research is noteworthy, highlighting its potential therapeutic applications.

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.