clk1 in 1

CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).

CLK1 2-IN-3(Cpd-3) 是一种具有高效性和选择性的 CLK1 和 CLK2 抑制剂，抗增殖活性，抑制 CLK1、CLK2、SRPK1、SRPK2、SRPK3 的 的活性。CLK1 2-IN-3 可诱导核斑点扩大，可诱导S6K pre-mRNA选择性剪接和随后抑制多种癌细胞类型细胞生长。

CLK1-IN-3 是一种+具有选择性和高效的性 Clk1 抑制剂，其 IC50 为 5 nM，比对 Dyrk1A 的亲和力高300对倍。CLK1-IN-3 对 Clk2 和 Clk4 也显示出高效的抑制作用，IC50 值分别为 42 和 108 nM。CLK1-IN-3 在体外有效诱导自噬 (autophagy)，可用于预防和人治疗急性肝损伤 (ALI)。

CLK1 2-IN-1 is a CLK1 and CLK2 inhibitor and it also inhibits SRPK1 and SRPK2.

CLK1 4-IN-1 (compound 31) is a highly potent and selective inhibitor of Clk1 and Clk4, with IC50 values of 9.7 nM and 6.6 nM, respectively. It effectively inhibits the growth of T24 cancer cells, with a GI50 value of 1.1 μM. CLK1 4-IN-1 has shown promising potential as an anticancer research tool [1].

DCLK1-IN-1 是选择性的、体内相容的双皮质素样激酶1（DCLK1）激酶结构域化学探针，也是一种高选择性的 DCLK1 2 抑制剂，通过结合和激酶测定IC50值分别为9.5 57.2 nM（DCLK1） 和 31 103 nM（DCLK2）。它具有低毒性，用于研究 DCLK1 生物学并确定其在癌症中的作用。

Mps1-IN-1 is a potent, selective and ATP-competitive inhibitor of Mps1 kinase (IC50 : 367 nM )

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.

Haspin-IN-2 (compound 4) 是一种有效的选择性的 haspin 抑制剂，IC50为 50 nM。Haspin-IN-1 还抑制 CLK1和DYRK1A，IC50分别为 445 nM 和 917 nM。

Haspin-IN-1 (compound 2a) 是一种haspin（单倍体生殖细胞特异性核蛋白激酶）抑制剂，IC50值为 119 nM。Haspin-IN-1 还抑制CLK1、DYRK1A 和 CDK9，IC50分别为 221 nM 、916.3 nM 和406.8 nM。Haspin-IN-1具有开发新型抗癌药物的潜力[1]。

CLK1-IN-2 是代谢稳定的Clk1抑制剂。CLK1-IN-2 对 Clk1 具有选择性，IC50值为 1.7 nM。CLK1-IN-2 可用于肿瘤、杜氏肌营养不良症和病毒感染如HIV-1和流感的研究。