[CAS NO. 3029431-68-0] CLK1-IN-2

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PRODUCTS SPECIFICATIONS [3029431-68-0]

Catalog

HY-152219

Brand

MCE

CAS

3029431-68-0

DESCRIPTION [3029431-68-0]

Overview

MDL	-
Molecular Weight	367.25
Molecular Formula	C16H12Cl2N2O2S
SMILES	O=C(C1=CC2=CC(OC)=CC=C2S1)NNC3=CC(Cl)=CC(Cl)=C3

For research use only. We do not sell to patients.

Summary

CLK1-IN-2 is metabolically stable Clk1 inhibitor. CLK1-IN-2 has selectivity for Clk1 with an IC ₅₀ 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] .

IC50 & Target

IC50: 1.7 nM (Clk1) ^[1] .

In Vitro

CLK1-IN-2 (Compound 27a) has selectivity for Clk1 with an IC ₅₀ 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 K _i valiue of 0.051 μM in NanoBRET cellular Clk1 engagement assay ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay ^[1]

Cell Line:	Human dermal fibroblasts
Concentration:	15 μM
Incubation Time:	2 days
Result:	Not affected the proliferation of normal human cells such as fibroblasts.

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Please store the product under the recommended conditions in the Certificate of Analysis.

References

[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.