DUB

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抑制剂选择性比较

特异性亚型抑制剂

DUB产品

所有产品 DUB抑制剂(16)

目录号	产品描述	文献引用	实验数据
S2243	Degrasyn (WP1130) Degrasyn (WP1130)是一种选择性deubiquitinase (DUB: USP5，UCH-L1，USP9x，USP14，和 UCH37)抑制剂，对Bcr/Abl也有抑制作用，也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。Degrasyn (WP1130)可诱导凋亡而阻滞自噬。	J Cell Mol Med, 2020, 24(2):1370-1382 J Biol Chem, 2020, 295(6):1694-1703 J Cell Biol, 2019, 218(7):2185-2197	Protein expression by western blot analysis of cell lysates from MCF-7, TAM^R-4 and 164^R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
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。	Nat Commun, 2020, 19;11(1):2487 Sci Adv, 2020, 26;6(9):eaay9269 Cell Rep, 2020, 5;31(5):107585	Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
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。	Mol Cell, 2020, 5;77(5):1124-1142 EMBO Rep, 2020, 3;21(4):e48978 Cell Immunol, 2020, 28;353:104115	Ubiquitination inhibitor PYR-41 and deubiquitination inhibitor PR-619 pretreated macrophages with or without Teuvincenone F (25 μM) for 2 h, following stimulated with LPS (100 ng/ml) for 30 min, and then subjected to immunoprecipitation with anti-NEMO antibody followed by immunoblot analysis with specific antibodies. Similar results were obtained from three independent experiments.
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。	Autophagy, 2020, 10.1080/15548627.2020.1740529 Genet Mol Biol, 2020, 20;43(2):e20190338 Cancer Discov, 2020, 22;CD-19-1436	(e) MM.1S cells were treated with RRx-001 (1.25 μM), P5091 (3 μM) or RRx-001 plus P5091 for 12 h; protein extracts were analyzed for total DNMT activity using the EpiQuik DNMT activity kit (mean±s.d.; P<0.001; n=3). (f) MM.1S cells were treated with RRx-001 (1.25 μM), P5091 (3 μM) or RRx-001 plus P5091 for 12 h; protein lysates were then subjected to immunoblot analysis using antibodies specific against p21, HDM2, p53 or GAPDH.
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。IU1可诱导自噬。	J Cell Mol Med, 2020, 10.1111/jcmm.15002 Nucleic Acids Res, 2020, 48(2):736-747 J Exp Clin Cancer Res, 2019, 38(1):220	IU1 treatment increased levels of peIF2a in both WT and S63del L. Sciatic nerves were treated ex vivo with 200 lM IU1 for 16 hr and the levels of p-eIF2a and eIF2a were analyzed by western blot. A Student’s t-test was performed between treated and untreated conditions of the same genotype
S6845^New	GRL0617 GRL0617 是一种有效的、选择性的、竞争性的重症急性呼吸综合征 (SARS-CoV) papain-like protease (PLPro)/deubiquitinase 的非共价抑制剂，其IC50值为0.6 μM、Ki值为0.49 μM。GRL0617 可抑制Vero E6细胞中的SARS-CoV病毒复制，对应的EC50值为15 microM，并且没有相关的细胞毒性。
S4922^New	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。
S8904^New	USP25/28 inhibitor AZ1 AZ1是一种非竞争性的泛素特异性蛋白酶25（USP25）和泛素特异性蛋白酶28（USP28）的双重抑制剂，在Ub-RH110检测中对USP25和USP28的IC50分别0.62 μM和0.7 μM。
S6748^New	ML364 ML364是去泛素化酶USP2的小分子抑制剂，IC50为1.1 μM（以含内部淬灭荧光双泛素为底物）。
S7135	LDN-57444 LDN-57444是一种可逆的竞争性的蛋白酶体抑制剂，抑制Uch-L1时，IC50为0.88 μM，比作用于亚型Uch-L3选择性高30倍。	Theranostics, 2020, 15;10(13):6048-6060 J Exp Clin Cancer Res, 2018, 37(1):258 J Cell Mol Med, 2017, 21(12):3641-3657	Representative results of Western blot showed the effects of LDN (10.0 μM) treatments on the expressions of LC3-II and LC3-I from Normoxia and OGD groups of cPKCc+/+ and cPKCc/ cortical neurons (n = 6 per group).
S7140	TCID TCID是一种DUB抑制剂，抑制ubiquitin C-terminal hydrolase L3（泛素C-末端水解酶L3），IC50为0.6 μM，作用于L1选择性高125倍。
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。	Cell Death Dis, 2020, 7;11(5):328 Br J Haematol, 2020, 4 Immunology, 2020, 159(3):309-321
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。	J Med Chem, 2020, 9;63(7):3756-3762 Front Mol Biosci, 2020, 22;7:49 Mol Cancer Ther, 2019, 18(6):1045-1056	A USP14 inhibitor directly inhibits OSCC cell proliferation and triggers apoptosis. (A-D) OSCC cells were treated with indicated doses of b-AP15 for 24 h. (A) Cell proliferation was monitored by CCK8 assay. b-AP15 dramatically decreased cancer cells viability in a dose-dependent manner (p < 0.01). All values represented means ± SD of three independent experiments and each was performed in triplicate. (B, C) Flow cytometry analysis indicated that b-AP15 triggered significant apoptosis of OSCC cells (p < 0.01). Data were obtained in more than three independent experiments. (D) Apoptosis-related proteins were examined by western blot analysis. Inhibition of USP14 with b-AP15 induced a massive increase of ubiquitinated proteins, which then triggered apoptosis of cancer cells, activating caspase 3 to induce cleavage of caspase 3 and PARP.
S7888	Spautin-1 Spautin-1是一种有效的特异性autophagy抑制剂，抑制USP10 和 USP13的去泛素化活性，IC50为∼0.6-0.7 μM。Spautin-1可增加凋亡。	J Cell Mol Med, 2020, 24(7):4324-4340 Autophagy, 2019, 15(2):312-326 Autophagy, 2019, 10.1080/15548627.2019.1628536	Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
S8288	VLX1570 VLX1570是蛋白酶DUB的竞争性抑制剂，在体外IC50值约为10μM。	J Med Chem, 2020, 9;63(7):3756-3762
S7529	ML323 ML323 是强效的选择性的USP1-UAF1抑制剂，其IC50为76 nM。	Cancer Sci, 2020, 10.1111 Mol Cell, 2018, 20;72(6):925-941.e4 Oncol Rep, 2017, 37(3):1419-1429

目录号	产品描述	文献引用	实验数据
S2243	Degrasyn (WP1130) Degrasyn (WP1130)是一种选择性deubiquitinase (DUB: USP5，UCH-L1，USP9x，USP14，和 UCH37)抑制剂，对Bcr/Abl也有抑制作用，也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。Degrasyn (WP1130)可诱导凋亡而阻滞自噬。	J Cell Mol Med,2020, 24(2):1370-1382 J Biol Chem,2020, 295(6):1694-1703 J Cell Biol,2019, 218(7):2185-2197	Protein expression by western blot analysis of cell lysates from MCF-7, TAM^R-4 and 164^R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
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。	Nat Commun,2020, 19;11(1):2487 Sci Adv,2020, 26;6(9):eaay9269 Cell Rep,2020, 5;31(5):107585	Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
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。	Mol Cell,2020, 5;77(5):1124-1142 EMBO Rep,2020, 3;21(4):e48978 Cell Immunol,2020, 28;353:104115	Ubiquitination inhibitor PYR-41 and deubiquitination inhibitor PR-619 pretreated macrophages with or without Teuvincenone F (25 μM) for 2 h, following stimulated with LPS (100 ng/ml) for 30 min, and then subjected to immunoprecipitation with anti-NEMO antibody followed by immunoblot analysis with specific antibodies. Similar results were obtained from three independent experiments.
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。	Autophagy,2020, 10.1080/15548627.2020.1740529 Genet Mol Biol,2020, 20;43(2):e20190338 Cancer Discov,2020, 22;CD-19-1436	(e) MM.1S cells were treated with RRx-001 (1.25 μM), P5091 (3 μM) or RRx-001 plus P5091 for 12 h; protein extracts were analyzed for total DNMT activity using the EpiQuik DNMT activity kit (mean±s.d.; P<0.001; n=3). (f) MM.1S cells were treated with RRx-001 (1.25 μM), P5091 (3 μM) or RRx-001 plus P5091 for 12 h; protein lysates were then subjected to immunoblot analysis using antibodies specific against p21, HDM2, p53 or GAPDH.
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。IU1可诱导自噬。	J Cell Mol Med,2020, 10.1111/jcmm.15002 Nucleic Acids Res,2020, 48(2):736-747 J Exp Clin Cancer Res,2019, 38(1):220	IU1 treatment increased levels of peIF2a in both WT and S63del L. Sciatic nerves were treated ex vivo with 200 lM IU1 for 16 hr and the levels of p-eIF2a and eIF2a were analyzed by western blot. A Student’s t-test was performed between treated and untreated conditions of the same genotype
S6845^New	GRL0617 GRL0617 是一种有效的、选择性的、竞争性的重症急性呼吸综合征 (SARS-CoV) papain-like protease (PLPro)/deubiquitinase 的非共价抑制剂，其IC50值为0.6 μM、Ki值为0.49 μM。GRL0617 可抑制Vero E6细胞中的SARS-CoV病毒复制，对应的EC50值为15 microM，并且没有相关的细胞毒性。
S4922^New	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。
S8904^New	USP25/28 inhibitor AZ1 AZ1是一种非竞争性的泛素特异性蛋白酶25（USP25）和泛素特异性蛋白酶28（USP28）的双重抑制剂，在Ub-RH110检测中对USP25和USP28的IC50分别0.62 μM和0.7 μM。
S6748^New	ML364 ML364是去泛素化酶USP2的小分子抑制剂，IC50为1.1 μM（以含内部淬灭荧光双泛素为底物）。
S7135	LDN-57444 LDN-57444是一种可逆的竞争性的蛋白酶体抑制剂，抑制Uch-L1时，IC50为0.88 μM，比作用于亚型Uch-L3选择性高30倍。	Theranostics,2020, 15;10(13):6048-6060 J Exp Clin Cancer Res,2018, 37(1):258 J Cell Mol Med,2017, 21(12):3641-3657	Representative results of Western blot showed the effects of LDN (10.0 μM) treatments on the expressions of LC3-II and LC3-I from Normoxia and OGD groups of cPKCc+/+ and cPKCc/ cortical neurons (n = 6 per group).
S7140	TCID TCID是一种DUB抑制剂，抑制ubiquitin C-terminal hydrolase L3（泛素C-末端水解酶L3），IC50为0.6 μM，作用于L1选择性高125倍。
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。	Cell Death Dis,2020, 7;11(5):328 Br J Haematol,2020, 4 Immunology,2020, 159(3):309-321
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。	J Med Chem,2020, 9;63(7):3756-3762 Front Mol Biosci,2020, 22;7:49 Mol Cancer Ther,2019, 18(6):1045-1056	A USP14 inhibitor directly inhibits OSCC cell proliferation and triggers apoptosis. (A-D) OSCC cells were treated with indicated doses of b-AP15 for 24 h. (A) Cell proliferation was monitored by CCK8 assay. b-AP15 dramatically decreased cancer cells viability in a dose-dependent manner (p < 0.01). All values represented means ± SD of three independent experiments and each was performed in triplicate. (B, C) Flow cytometry analysis indicated that b-AP15 triggered significant apoptosis of OSCC cells (p < 0.01). Data were obtained in more than three independent experiments. (D) Apoptosis-related proteins were examined by western blot analysis. Inhibition of USP14 with b-AP15 induced a massive increase of ubiquitinated proteins, which then triggered apoptosis of cancer cells, activating caspase 3 to induce cleavage of caspase 3 and PARP.
S7888	Spautin-1 Spautin-1是一种有效的特异性autophagy抑制剂，抑制USP10 和 USP13的去泛素化活性，IC50为∼0.6-0.7 μM。Spautin-1可增加凋亡。	J Cell Mol Med,2020, 24(7):4324-4340 Autophagy,2019, 15(2):312-326 Autophagy,2019, 10.1080/15548627.2019.1628536	Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
S8288	VLX1570 VLX1570是蛋白酶DUB的竞争性抑制剂，在体外IC50值约为10μM。	J Med Chem,2020, 9;63(7):3756-3762
S7529	ML323 ML323 是强效的选择性的USP1-UAF1抑制剂，其IC50为76 nM。	Cancer Sci,2020, 10.1111 Mol Cell,2018, 20;72(6):925-941.e4 Oncol Rep,2017, 37(3):1419-1429