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Cat. No. Product Name CAS No. Information
PC-35047

T-025

T-025 (T025, CLK inhibitor T-025) is an orally available, potent inhibitor of Cdc2-like kinases (CLKs) with Kd of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, also inhibits DYRK1A and DYRK1B with IC50 of 0.074 and 1.5 nM; reduces CLK-dependent phosphorylation, induces skipping exon, resulting in anti-proliferative effect in MDA-MB-468 in vitro and in vivo accompanied by the modulation of pre-mRNA splicing; shows sensitivity against high CLK2 expression or MYC amplification cancer celles; exhibits significant anti-tumor efficacy in MYC-driven breast tumor allograft models.

PC-61023

TG693

885272-55-9

TG693 is an orally available, selective, ATP-competitive CLK1 inhibitor with IC50 of 112.6 nM; also potently inhibits haspin activity and weakly inhibits DYRK kinases in a panel of 313 recombinant kinases; promotes the skipping of the endogenous mutated exon 31 in DMD patient-derived cells and increases the production of the functional exon 31-skipped dystrophin protein; inhibits the phosphorylation of CLK1 substrate serine/arginine-rich proteins and modulates pre-mRNA splicing in the skeletal muscle in mice.

PC-61021

CLK inhibitor T3

2109805-56-1

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.

PC-35359

CLK2 inhibitor Indazole1

CLK2 inhibitor Indazole1 is a novel potent, selective inhibitor of CLK2 with IC50 of 2.7 nM, 60-fold selectivity over PKA and >600-fold selectivity over a panel of 34 kinases; rescues spine density in mouse brain slices at 300 nM; displays 96-fold more potent than TG003 in the CLK2 Caliper assay.
PC-63478

Leucettamine B

147395-96-8 Leucettamine B is a potent inhibitor of CLK1 (IC50=15 nM), Dyrk1A (IC50=40 nM), and Dyrk2 (IC50=35 nM) and a moderate inhibitor of CLK3 (IC50=4.5 uM).
PC-63477

ML197

1222891-88-4 ML197 is a potent, selective small molecule inhibitor of Cdc2-like kinases (CLK) and DYRK with IC50 of 96/40/206 nM for CLK1/CLK4/Dyrk1A, respectively; inhibits CLK2, CLK3 and Dyrk1B with IC50 of 1327, 7448 and 1510 nM, extends intracellular NKX3.1 half-life in LNCaP prostate cancer cells;
PC-63470

KuWal151

KuWal151 is a potent, selective cdc2-like kinase (CLK) inhibitor with IC50 of 88/510/28 nM for CLK1/2/4, respectively; shows no activity against CLK3 (IC50>10 uM), exhibits selectivity versus DYRK1A and other DYRK kinases; displays a potent antiproliferative activity in an array of cultured cancer cell lines (HCT-116 cell GI50=191 nM).

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