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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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