clk3

T025 是一种泛 CLK 抑制剂，对 CLK1-4 的 Kd 分别为 4.8、0.096、6.5、0.61 和 0.074 nM。 T025 在血液学和实体癌细胞系中表现出抗增殖活性，IC50 为 30-300 nM。 T025 可用于 MYC 驱动疾病的研究。

CLK-IN-T3 是 CLK1、CLK2 和 CLK3 的抑制剂，IC50 为 0.67、15 和 110 nM。 CLK-IN-T3 具有抗癌活性。

K 00546 是一种高效性细胞周期性蛋白激酶（CDK1 和 CDK2）和CDC2 样激酶（CLK1 和 CLK3） 抑制剂，可用于研究癌症和免疫相关疾病。

KH-CB19 is an effective and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1 CLK4).

PfCLK3-IN-1（Compound 4）作为恶性疟原虫CLK3（Pf CLK3）的共价抑制剂，在碱性环境中效果显著，其pEC50值达7.1。该化合物能够有效减少恶性疟原虫在性阶段的配子体成熟，进而阻断疾病的传播。此外，PfCLK3-IN-1对恶性疟原虫Dd2-B2克隆具有抑制作用，其IC50值为239.5 nM。

Leucettine L41 (LeucettineL41) 是优先作用于 DYRK1A 的 DYRKs CLKs 抑制剂，抑制 DYRK2、CDC 样激酶1 (CLK1) 和 CLK3，诱导与 CLK 抑制相关的自噬。Leucettine L41 可用于研究阿尔茨海默病和记忆缺陷。

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5 6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265

KH-CB20, an E Z mixture, is a potent and selective inhibitor of CLK1 and CLK4 , with an IC 50 of 16.5 nM for CLK1 . KH-CB20 also can inhibits DYRK1A ( IC 50 =57.8 nM) and CLK3 ( IC 50 =488 nM).

Leucettinib-92（化合物92）作为DYRK CLK激酶家族的抑制剂，展现出对多种激酶具有不同程度的抑制活性，IC50s依次为CLK1 147 nM、CLK2 39 nM、CLK4 5.2 nM、CLK3 0.8 μM、DYRK1A 124 nM、DYRK1B 204 nM、DYRK2 0.16 μM、DYRK3 1.0 μM、DYRK4 0.52 μM、GSK3 2.78 μM。

ZJCK-6-46 (32) 是一种拥有口服活性的潜在DYRK1A抑制剂,IC50 值为0.68 nM,且具备良好的CNC通透性.此化合物能有效降低tau蛋白的磷酸化水平,并通过显著降低磷酸化tau蛋白的表达及减少神经元损失,从而改善认知功能障碍.