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PYR-41 是一种选择性,可透过细胞的泛素活化酶 E1抑制剂,IC50值小于10 μM。
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PYR-41 是一种选择性,可透过细胞的泛素活化酶 E1抑制剂,IC50值小于10 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 288 | 现货 | |
5 mg | ¥ 496 | 现货 | |
10 mg | ¥ 828 | 现货 | |
25 mg | ¥ 1,460 | 现货 | |
50 mg | ¥ 2,370 | 现货 | |
100 mg | ¥ 3,530 | 现货 | |
200 mg | ¥ 5,120 | 现货 | |
500 mg | ¥ 7,830 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 552 | 现货 |
产品描述 | PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. |
靶点活性 | E1:< 10 μM |
体外活性 | PYR-41 (50 μM) inhibits activity of ubiquitin-activating enzyme E1 by over 90%. PYR-41 could be a target for nucleophilic attack and potentially reacts with the active site cysteine of E1. PYR-41 efficiently blocks cyclin E degradation. PYR-41 decreases the level of E1fUb thioesters in cells with a IC50 of between 10 and 25 μM, and prevents proteasome inhibitor–induced accumulation of ubiquitylated proteins. PYR-41 increases total sumoylation in cells and in cell harboring temperature-sensitive E1. PYR-41 is able to inhibit both proteasome-dependent and proteasome-independent activities of ubiquitylation. PYR-41 (50 μM) attenuates 1 ng/mL IL-1α-mediated nuclear factor-κB activation by >60% through preventing the downstream ubiquitylation and proteasomal degradation of IκBα. PYR-41 inhibits degradation of p53 and activates the transcriptional activity of p53, which enable its differentially killing transformed p53-expressing cells. [1] PYR-41 blocks ubiquitination reactions but paradoxically leads to the accumulation of high MW ubiquitinated proteins. PYR-41 also has equal or greater inhibitory activity against several deubiquitinases (DUBs) in intact cells and purified USP5 in vitro. PYR-41 also mediates cross-linking of specific protein kinases (Bcr-Abl, Jak2) to inhibit their signaling activity. [1] |
激酶实验 | Rabbit or mouse E1 (apper 250 ng) is incubated with 32P-ubiquitin in 1× reaction buffer [50 mM Tris (pH 7.4), 0.2 mM ATP, 0.5 mM MgCl2] at room temperature for 15 min. In some experiments, the His-tagged mouse E1 is bound to TALON cobalt affinity resin before carrying out incubations and reactions. Mouse E1 and 32P-ubiquitin are added to the beads in 1× reaction buffer and incubated as for E1 reactions. Samples are heated in nonreducing SDS-PAGE sample buffer and resolved by SDS-PAGE. Thioesters with ubiquitin are visualized by Storm PhosphoImager. |
别名 | PYR41, PYR 41 |
分子量 | 371.3 |
分子式 | C17H13N3O7 |
CAS No. | 418805-02-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 5.5 mg/mL (14.81 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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