CLKs (Cdc2-like kinase) are dual specificity protein kinases which are involved in gene splicing regulation. The CLK family has four family members: CLK1/STY, CLK2, CLK3 and CLK4. CLKs are useful targets for studying diseases attributed to gene mis-splicing events.
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KH-CB19 is a potent and highly specific inhibitor of CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4) with IC50 of 20 nM (CLK1), displays almost 100-fold selectivity against the CLK3 isoform; effectively suppresses phosphorylation of SR (serine/arginine) proteins SRp75 and SRp55 in cells; significantly reduces the basal expression of flTF as well as asHTF, also lowers TNF-α-induced expression of both TF mRNA splice variants to baseline in HMEC-1 cells.
MU1210 (MU-1210) is a potent and highly selective inhibitor of cdc-like kinases (CLKs) with IC50 of 51 nM (cellular BRET for CLK1); profoundly affected the Mdm4 alternative splicing and showed high activity in cytotoxicity assays using MCF7 breast cancer cells; MU1210 has favorable pharmacokinetics (mouse, 10 mpk, IP: Cmax =1.24 mm, T1/2 = 58 min; no acute toxicity observed), suggesting its potential use in in vivo models; MU1210 is a quality probe for CLK1, CLK2, and CLK4.
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;
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).
CLK inhibitor T3
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
A potent, selective CDC-like kinase 4 (CLK4) inhibitor with IC50 of 136 nM, >10-fold selectivity over Clk1, Clk2, Clk3, Dyrk1A/1B.
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.
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.
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).
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.
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