CUR61414 是一种新型的可渗透细胞的 Hedgehog 信号通路抑制剂 (IC50 =100-200 nM)，CUR61414 是氨基脯氨酸类化合物的小分子成员，可选择性结合 Smoothened (Smo)，Ki 值为 44 nM。CUR-61414可以诱导癌细胞凋亡 (apoptosis) 而不会影响非癌症细胞。
| 生物活性 |
CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells. |
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| 体外研究 |
CUR61414 is able to arrest proliferation of basal cells within the BCC-like lesions and induce cells to undergo apoptosis resulting in complete regression of the lesions, without affecting neighboring skin cells. |
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| 体内研究 |
CUR61414 cause regression of these lesions in the mice, which are exposed to UV light irradiation for 6-9 months, producing many microscopic BCC-like basaloid lesions throughout their skin. Moreover,a significant increase in apoptotic nuclei can be seen in basaloid nests after CUR61414 treatment and no overt toxicity is observed in the skin surrounding the lesions.
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| 分子式 |
C31H42N4O5
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| 分子量 |
550.69
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| CAS号 |
334998-36-6
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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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| 科研文献 |
纯度： 98%
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