TAK-243 | MedChemExpress (MCE)-产品咨询-资讯-生物在线

TAK-243 | MedChemExpress (MCE)

作者:MedChemExpress LLC 暂无发布时间 (访问量:1273)

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TAK-243

CAS No. : 1450833-55-2

MCE 国际站:TAK-243

产品活性:TAK-243 (MLN7243) 是一种首创的,选择性的泛素激活酶,UAE (UBA1) 抑制剂 (IC50=1 nM),其阻断了泛素结合,破坏了单泛素信号传导和全蛋白泛素化。TAK-243 (MLN7243) 诱导内质网应激 (ERS) 反应,消除 NF-κB 通路活化,促进细胞凋亡。

研究领域:Metabolic Enzyme/Protease  |  NF-κB  |  Apoptosis

作用靶点:E1/E2/E3 Enzyme  |  NF-κB  |  Apoptosis

In Vitro: TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 μM to 1.31 μM.
?TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours.

In Vivo: TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity.

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