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.

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].

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.

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.

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]

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.

OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8. OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung cancer.

USP7-797 is a selective non-covalent active site USP7 inhibitor, inhibiting USP7 and ubiquitin binding, with anti-tumor, oral and high efficiency (IC50=0.44 nmol), it is effective on both wild-type and mutant p53 tumor cells, and can significantly inhibit the growth of tumor cells and induce apoptosis.

USP28-IN-3 is a highly selective USP28 inhibitor with an IC50 value of 0.1 μM against USP28.USP28-IN-3 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3, and UCHL5.USP28-IN-3 is cytotoxic to human colorectal and lung squamous carcinoma cells, inhibiting c-cells and c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-cells through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

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.

FT827 is a covalent inhibitor of selective ubiquitin-specific protease 7 (USP7) (Ki=4.2 µM, Kd=7.8 µM) targeting the catalytic center of the autoinhibitory apolipoprotein form of USP7 for cancer research.

RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs) with a favorable toxicity profile and anticancer activity, particularly effective in inducing apoptosis in ovarian cancer cell lines.