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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-NEDD8-TAS4464
TAS4464

Chemical Structure : TAS4464

CAS No.: 1848959-10-3

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TAS4464 (TAS-4464)

货号: PC-72994Not For Human Use, Lab Use Only.

TAS4464 (TAS-4464) is a highly potent and selective inhibitor of NEDD8-activating enzyme (NAE) with IC50 of 0.955 nM, >400-fold selectivity over UAE and SAE.

规格 价格 库存 数量
5 mg ￥1480 In stock
10 mg ￥2180 In stock
25 mg ￥3780 In stock
50 mg ￥5780 In stock
100 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

TAS4464 (TAS-4464) is a highly potent and selective inhibitor of NEDD8-activating enzyme (NAE) with IC50 of 0.955 nM, >400-fold selectivity over UAE and SAE.
TAS4464 functionally inhibits NAE and that this inhibitory activity is more potent and more selective than that of MLN4924, and does not inhibit Carbonic anhydrase II (CA2, IC50=0.73 uM).
TAS4464 (dose range, 0.001-1 μmol/L) induced dose-dependent decreases in neddylated cullin and dose-dependent accumulation of the CRL substrates CDT1, NRF2, p-IκBα, and p27 in the human cancer cell line CCRF-CEM.
TAS4464 increased the levels of cleaved caspase-3 and cleaved PARP, did not induce the accumulation of the non-CRL substrates such as GADD34 and PTTG.
TAS4464 exhibited strong and sustained neddylation inhibition and caused profound antitumor efficacy in CCRF-CEM xenograft model.

物理化学性质&存储条件

分子量 506.509
分子式 C21H23FN6O6S
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

7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[5-[(aminosulfonyl)amino]-5-deoxy-beta-D-ribofuranosyl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]-

参考文献

1. Yoshimura C, et al. Mol Cancer Ther. 2019 Jul;18(7):1205-1216.

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