| Bioactivity | CLK1-IN-2 is metabolically stable Clk1 inhibitor. CLK1-IN-2 has selectivity for Clk1 with an IC50 value of 1.7 nM. CLK1-IN-2 can be used for the research of tumour, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza[1]. | ||||||||||||
| Target | IC50: 1.7 nM (Clk1). | ||||||||||||
| Invitro | CLK1-IN-2 (Compound 27a) 对 Clk1 具有选择性，IC50 值为 1.7 nM[1]。CLK1-IN-2 的代谢半衰期长达 6.4 小时[1]。CLK1-IN-2 在 T24 癌细胞中的 GI50 为 3.4 μM[1]。CLK1-IN-2 在 NanoBRET 细胞 Clk1 结合测定中显示细胞 Ki 值为 0.051 μM[1]。 Cell Cytotoxicity Assay[1] Cell Line: | ||||||||||||
| Name | CLK1-IN-2 | ||||||||||||
| Formula | C16H12Cl2N2O2S | ||||||||||||
| Molar Mass | 367.25 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Dalia S El-Gamil, et al. Discovery of novel 5-methoxybenzothiophene hydrazides as metabolically stable Clk1 inhibitors with high potency and unprecedented Clk1 isoenzyme selectivity. Eur J Med Chem. 2022 Dec 15;247:115019. |