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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-activating Enzyme (E1)-PYR-41
PYR-41

Chemical Structure : PYR-41

CAS No.: 418805-02-4

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PYR-41 (PYR41, PYR 41)

货号: PC-43474Not For Human Use, Lab Use Only.

PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM.

规格 价格 库存 数量
10 mg ￥880 In stock
25 mg ￥1580 In stock
50 mg ￥2480 In stock
100 mg ￥3980 In stock
200 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM.
PYR-41 does not affect the transfer of ubiquitin to E2 from E1, directly inhibits E1, but not E2.
In addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells, attenuates cytokine-mediated nuclear factor-kappaB activation and inhibits nonproteasomal (Lys-63) ubiquitylation of TRAF6, also prevents the downstream ubiquitylation and proteasomal degradation of IκBα。
PYR-41 inhibits degradation of p53 and activates the p53 transcriptional activity, demonstrates anti-tumor activity in animal studies.

物理化学性质&存储条件

分子量 371.30
分子式 C17H13N3O7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 46 mg/mL
Chemical Name/SMILES

Benzoic acid, 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-, ethyl ester

参考文献

1. Yang Y, et al. Cancer Res. 2007 Oct 1;67(19):9472-81.

2. Kapuria V, et al. Biochem Pharmacol. 2011 Aug 15;82(4):341-9.

3. Chen C, et al. Immunology. 2014 Jun;142(2):307-19.

4. Matsuo S, et al. Shock. 2018 Apr;49(4):442-450.

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