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Product introduction

MLN4924是一种有效的和选择性的NEDD8激活酶（NAE）抑制剂，IC50值为4 nM。 MLN4924与AMP竞争结合NAE的核苷酸结合位点。与密切相关的酶UAE、SAE、UBA6和ATG7（IC50值分别为1.5、8.2、1.8和10 μM）相比，MLN4924对NAE具有高选择性。MLN4924对其它利用ATP的酶没有作用。在HCT-116细胞中，MLN4924导致Ubc12-NEDD8硫酯和NEDD8-滞蛋白（cullin）缀合物的减少，从而抑制CRL-泛素化介导的蛋白降解（比如CDT1蛋白），CDT1蛋白的积累会引起细胞周期缺陷。在HCT-116异种移植小鼠中，MLN4924以30 mg/kg和60 mg/kg的剂量显著抑制肿瘤生长，这些剂量的耐受性良好。在H522和Calu-6肺癌异种移植小鼠中，MLN4924也具有抗肿瘤活性。 Pevonedistat (MLN4924)是Nedd8激活酶(NAE)的小分子抑制剂，IC50为4 nM。

Specs ⸢ View details ⸥

Chinese name

MLN4924,NEDD8活化酶抑制剂, NEDD8 激活酶抑制剂

English name

MLN4924

Chinese alias

((1S,2S,4R)-4-(4-(((S)-2,3-二氢-1H-茚-1-基)氨基)-7H-吡咯并[2,3-d]嘧啶-7-基)-2-羟基环戊基)甲基氨基磺酸酯

English alias

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 | Pevonedistat

CAS number

905579-51-3

molecular formula

C21H25N5O4S

molecular weight

443.53 g/mol

Exact mass

PSA

141.000 Å²

Logp

1.7

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Pevonedistat (MLN4924) 99% 1mg

Name: Pevonedistat (MLN4924) 99% 1mg
Brand: 麦克林
SKU: P872287-1mg

Pevonedistat (MLN4924) 99% 1mg CAS 905579-51-3, complete specifications for production, research, laboratory testing and inspection; digital one-stop procurement platform for scientific materials.

item number：P872287-1mg

Product model：1mg

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Lead Time：30days

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Pevonedistat (MLN4924) 99% 1mg

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