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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-activating Enzyme (E1)-IJ-5
IJ-5

Chemical Structure : IJ-5

CAS No.: 68776-47-6

IJ-5 (IJ5;IJ 5;1beta-Hydroxyalantolactone)

货号: PC-60355Not For Human Use, Lab Use Only.

A potent, covalent inhibitor of ubiquitin-conjugating enzyme UbcH5 with Kd of 5.189 uM, 3.578 uM, and 2.577 uM for UbcH5a, UbcH5b, and UbcH5c, respectively.

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5 mg ¥4580 In stock
10 mg ¥7880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

IJ-5 (1beta-Hydroxyalantolactone) is a potent, covalent inhibitor of ubiquitin-conjugating enzyme UbcH5 with Kd of 5.189 uM, 3.578 uM, and 2.577 uM for UbcH5a, UbcH5b, and UbcH5c, respectively.
IJ-5 shows weak affinity for Ubc13 (Kd=13.37 uM); inhibits TNFα-induced NF-kB pathway activation and inflammatory gene expression in 293T cells.
IJ-5 exhibites potent anti-inflammatory activity against TNF-α- and D-galactosamine-induced hepatitis and collagen-induced arthritis in preclinical models.

物理化学性质&存储条件

分子量 248.322
分子式 C15H20O3
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

10 mM in DMSO

Chemical Name/SMILES

(3aS,5R,8S,8aS,9aS)-8-hydroxy-5,8a-dimethyl-3-methylene-3a,5,6,7,8,8a,9,9a-octahydronaphtho[2,3-b]furan-2(3H)-one

参考文献

1. Liu L, et al. Chem Biol. 2014 Oct 23;21(10):1341-50.

2. Chen H, et al. J Med Chem. 2017 Jul 11. doi: 10.1021/acs.jmedchem.6b01829.

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