INDY 是一种有效，ATP 竞争性的 Dyrk1A 和 Dyrk1B 抑制剂，IC50 分别为 0.24 μM 和 0.23 μM。INDY 结合在酶的 ATP 口袋中，对 Dyrk1A 的 Ki 值为 0.18 μM。INDY 大大降低了原代胶质母细胞瘤 (GBM) 细胞系和神经祖细胞中正常细胞和致瘤细胞的自我更新能力。
| 生物活性 |
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells. |
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| 体外研究 |
INDY (0.3-30 μM; 20 hours) mildly inhibits tau-phosphorylation at 3 μM, and nearly completely inhibits at 30 μM. Western Blot Analysis
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| 体内研究 |
ProINDY (2.5 μM) recoveres apparently normal development of the Xenopus embryo.
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| 分子式 |
C12H13NO2S
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| 分子量 |
235.30
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| CAS号 |
1169755-45-6
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： ≥98%
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