DUB
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
DUB产品
| 产品目录 | 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)。 |
Protein expression by western blot analysis of cell lysates from MCF-7, TAMR-4 and 164R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
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| S7130 |
PR-619PR-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。 |
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.
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| 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。 |
(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.
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| S7134 |
IU1IU1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 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
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| S7135 |
LDN-57444LDN-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。 |
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).
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| S7140 |
TCIDTCID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。 |
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| S7133 |
P22077P22077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。 |
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| S4920 |
b-AP15b-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。 |
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.
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| S8288 |
VLX1570VLX1570是蛋白酶DUB的竞争性抑制剂，在体外IC50值约为10μM。 |
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| S7529 |
ML323ML323 是强效的选择性的USP1-UAF1抑制剂，其IC50为76 nM。 |
| 产品目录 | 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)。 |
Protein expression by western blot analysis of cell lysates from MCF-7, TAMR-4 and 164R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
|
|
| S7130 |
PR-619PR-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。 |
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。 |
(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 |
IU1IU1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 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
|
|
| S7135 |
LDN-57444LDN-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。 |
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 |
TCIDTCID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 |
P22077P22077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。 |
||
| S4920 |
b-AP15b-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。 |
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.
|
|
| S8288 |
VLX1570VLX1570是蛋白酶DUB的竞争性抑制剂，在体外IC50值约为10μM。 |
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| S7529 |
ML323ML323 是强效的选择性的USP1-UAF1抑制剂，其IC50为76 nM。 |
