USP/UBP 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8967 XL177A

XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.

Selective USP7, IC50: 0.34 nM
S6878 GSK2643943A

GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho.

Selective USP20/Ub-Rho, IC50: 160 nM
S2913 BAY 11-7082

BAY 11-7082是一种NF-κB抑制剂,抑制TNFα诱导的IκBα磷酸化,在肿瘤细胞中IC50为10 μM。同时对泛素化系统的组分也有抑制作用。

Selective USP6, IC50: 1.7 μM; USP21, IC50: 0.96 μM; USP7, IC50: 0.19 μM
S7888 Spautin-1

Spautin-1是一种有效的特异性autophagy抑制剂,抑制USP10USP13的去泛素化活性,IC50为∼0.6-0.7 μM。

Selective USP10, IC50: 0.5779 μM; USP13, IC50: 0.6916 μM
S6933 GEN-6776

GNE-6776 is a potent, non-covalent, selective and orally bioavailable inhibitor of USP7 with IC50 of 1.34 μM and 0.61 μM for full length USP7 and USP7 catalytic domain, respectively.

Selective USP7 catalytic domain, IC50: 0.61 μM; full length USP7, IC50: 1.34 μM
S8904 USP25/28 inhibitor AZ1

AZ1 is a potent and noncompetitive dual Inhibitors of the ubiquitin-specific protease (USP) 25/28 with IC50s of 0.62 μM and 0.7 μM in Ub-RH110 assay,respectively.

Selective USP28, IC50: 0.7 μM; USP25, IC50: 0.62 μM
S6748 ML364

ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.

Selective USP8, IC50: 0.95 μM; USP2, IC50: 1.1 μM
S7132 P5091 (P005091)

P5091 (P005091)是一种选择性的,有效的ubiquitin-specific protease 7 (USP7)(泛素特异性蛋白酶7)抑制剂,EC50为4.2 μM,与作用于USP47相似。

Selective USP47, IC50: 4.3 μM; USP7, EC50: 4.2 μM
S7134 IU1

IU1是一种细胞渗透性的,可逆的proteasome(蛋白酶体)选择性抑制剂,作用于USP14时,IC50为4.7 μ M,作用于IsoT时 选择性高25倍。

Selective USP14, IC50: 4.7 μM
S7133 P22077

P22077是一种ubiquitin-specific protease USP7(泛素特异性蛋白酶USP7)抑制剂,EC50为8.6 μM,也抑制USP47

Selective USP47, EC50: 8.74 μM; USP7, IC50: 8.6 μM
S4922 NSC 632839

NSC 632839不仅是一种DUB抑制剂,也是一种deSUMOylase抑制剂,作用于USP2, USP7,和SENP2, IC50分别为45 μM, 37 μM和9.8 μM。

Selective USP7, EC50: 37 μM; USP2, EC50: 45 μM
S6877 EOAI3402143

EOAI3402143 is a dose-dependent inhibitor of Usp9x, Usp24 and Usp5 that increases tumor cell apoptosis, and fully blocks or regresses myeloma tumors in mice.

Selective
S7130 PR-619

PR-619是一种非选择性的,deubiquitinylating enzymes (DUBs)可逆抑制剂,无细胞试验中EC50为1-20 μM。

Pan USP47, EC50: 8.87 μM; USP28, EC50: 6.24 μM; USP20, EC50: 5.10 μM; USP15, EC50: 8.23 μM; USP8, EC50: 4.90 μM; USP7, EC50: 6.86 μM; USP5, EC50: 8.61 μM; USP4, EC50: 3.93 μM; USP2 core, EC50: 7.20 μM
S4920 b-AP15

b-AP15是一种deubiquitinases(去泛素化酶)抑制剂,识别19S蛋白酶体的,抑制Ub-AMC分解, IC50为2.1 μM。

Pan