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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-NEDD8-MLN4924 hydrochloride
MLN4924 hydrochloride

Chemical Structure : MLN4924 hydrochloride

CAS No.: 1160295-21-5

MLN4924 hydrochloride (Pevonedistat hydrochloride, TAK-924 hydrochloride)

货号: PC-42613Not For Human Use, Lab Use Only.

MLN4924 (Pevonedistat) hydrochloride is an analog of adenosine 5’-monophosphate that potently and selectively inhibits NEDD8-activating enzyme (NAE) with IC50 of 4.7 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MLN4924 (Pevonedistat) hydrochloride is an analog of adenosine 5’-monophosphate that potently and selectively inhibits NEDD8-activating enzyme (NAE) with IC50 of 4.7 nM.
MLN4924 also inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 of 1.5 and 8.2 uM, respectively.
MLN4924 disrupts CRL-mediated protein turnover leading to apoptosis in HCT116 cells.
MLN4924 suppresses the growth of human tumor xenografts in mice (30-60 mg/kg).

物理化学性质&存储条件

分子量 479.9803
分子式 C21H26ClN5O4S
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: ≥ 160 mg/mL

Chemical Name/SMILES

Sulfamic acid, [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl ester, hydrochloride (1:1)

参考文献

1. Soucy TA, et al. Nature. 2009 Apr 9;458(7239):732-6.

2. Milhollen MA, et al. Blood. 2010 Sep 2;116(9):1515-23.

3. Brownell JE, et al. Mol Cell. 2010 Jan 15;37(1):102-11.

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