CLK inhibitor T3

Research use only, not for human use.

CLK inhibitor T3 (T3) is a highly potent, selective, and cell-based stable CDC-like kinase (CLK) inhibitor with 0.67, 15 and 110?nM for CLK1,2 and 3, respectively.

CLK inhibitor T3 (T3) is a highly potent, selective, and cell-based stable CDC-like kinase (CLK) inhibitor with 0.67, 15 and 110?nM for CLK1,2 and 3, respectively; displays 200-300-fold selectivity over other dual specificity kinases such as DYRK1A and DYRK1B; induces dose-dependent reduction in exon recognition and exhibits an overlapping, but greater effect on transcriptome splicing compared to KH-CB19.

CLK-IN-T3 inhibits DYRK1A (IC50=260 nM) and DYRK1B (IC50=230 nM). CLK-IN-T3 (0.1-10.0 μM; 24 hours) results in mild cell cycle arrest at the G2/M boundary with long-duration (24 h). CLK-IN-T3 (0.5-1.0 μM; 6 hours) decreases phosphorylation of CLK-targeted SR proteins and CLK proteins increase slightly. Cell Cycle Analysis Cell Line:HCT-116 cells.Concentration:0.1, 0.5, 1.0, 5.0, 10.0 μM Incubation Time:24 hours Result:Resulted in mild cell cycle arrest at the G2/M boundary with long-duration (24 h).Western Blot Analysis Cell Line:HCT-116 cells Concentration:0.5, 1.0 μM Incubation Time:6 hours Result:Decreased phosphorylation of CLK-targeted SR proteins and CLK proteins increased slightly.

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T3

Cell Cycle/DNA Damage

CLK

CLK

Cancer

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2109805-56-1

482.588

C28H30N6O2

>98% (HPLC)

In Vitro:?DMSO : 4.83 mg/mL (10.01 mM)

O=C(NC1=CN2C=C(C3=CC=NC=C3)C=CC2=N1)C4=CC=C(C(C)(C)C(N5CCN(C)CC5)=O)C=C4

4-(2-methyl-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl)-N-(6-(pyridin-4-yl)imidazo[1,2-a]pyridin-2-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years