CLK1-IN-2

• CAT Number: I042355
• CAS Number: 3029431-68-0
• Molecular Formula: C16H12Cl2N2O2S
• Molecular Weight: 367.25
• Purity: ≥95%
• Synonyms: N’-(3,5-dichlorophenyl)-5-methoxy-1-benzothiophene-2-carbohydrazide
• InChI: InChI=1S/C16H12Cl2N2O2S/c1-22-13-2-3-14-9(4-13)5-15(23-14)16(21)20-19-12-7-10(17)6-11(18)8-12/h2-8,19H,1H3,(H,20,21)
• InChIKey: ZDJFIKFQLKJRBA-UHFFFAOYSA-N
• SMILES: COC1=CC2=C(C=C1)SC(=C2)C(=O)NNC3=CC(=CC(=C3)Cl)Cl

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].
CLK1-IN-2 (Compound 27a) has selectivity for Clk1 with an IC50 value of 1.7 nM[1].
CLK1-IN-2 shows long metabolic half-lives of 6.4 h[1].
CLK1-IN-2exhibits a GI50 of 3.4 μM in T24 cancer cells[1].
CLK1-IN-2 shows a cellular Ki valiue of 0.051 μM in NanoBRET cellular Clk1 engagement assay[1].

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.
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