DUB
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S2243 | Degrasyn (WP1130) | <1 mg/mL | 77 mg/mL | 18 mg/mL |
| S7130 | PR-619 | <1 mg/mL | 45 mg/mL | <1 mg/mL |
| S7132 | P5091 (P005091) | <1 mg/mL | 28 mg/mL | <1 mg/mL |
| S7134 | IU1 | <1 mg/mL | 60 mg/mL | 60 mg/mL |
| S7135 | LDN-57444 | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S7140 | TCID | <1 mg/mL | 23 mg/mL | <1 mg/mL |
| S7133 | P22077 | <1 mg/mL | 63 mg/mL | <1 mg/mL |
| S4920 | b-AP15 | <1 mg/mL | 48 mg/mL | <1 mg/mL |
| S8288 | VLX1570 | <1 mg/mL | 93 mg/mL | <1 mg/mL |
| S7529 | ML323 | <1 mg/mL | 76 mg/mL | 38 mg/mL |
特异性亚型抑制剂
- DUB抑制剂（10）
| 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)。 |
HEK-293 cells expressing Strep-CLASPIN were first arrested in S-phase with HU or in mitosis with nocodazole. Cycloheximide was then added to prevent further protein synthesis in the presence or absence of the USP9X inhibitor WP1130 and samples were harvested at the indicated times. A sample from the same cell line uninduced (U) was loaded as control.
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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。 |
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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。 |
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