clk1

CLK1/2-IN-3 (Cpd-3) is a potent and selective CLK1 and CLK2 inhibitor with antiproliferative activity and inhibits the activities of CLK1, CLK2, SRPK1, SRPK2, and SRPK3.CLK1/2-IN-3 induces nuclear speckle enlargement, which induces S6K pre-mRNA-selective splicing and subsequent inhibition of cell growth of multiple cancer cell types. cancer cell types cell growth.

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).

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

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

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025 can be used in studies about MYC-driven diseases.

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

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

K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases.

ML167 (CID44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.

TG003 is a potent Clk1/Sty inhibitor that inhibits Clk1 and Clk4, inhibits cancer cell growth and induces apoptosis, and can be used in the study of Duchenne muscular dystrophy.

WAY-322243 has antibacterial and anti-inflammatory activity and has an inhibitory effect on CLK-1, which can be used to study Alzheimer's disease.

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].

CLK1-IN-2, a metabolically stable Clk1 inhibitor, exhibits selective activity for Clk1 with an IC50 value of 1.7 nM. It is applicable in researching tumor, Duchenne's muscular dystrophy, and viral infections including HIV-1 and influenza.

MDK6204 is a selective inhibitor of CLK1 and CLK2.

DCLK1-IN-3 is a potent and selective inhibitor of doublecortin-like kinase 1 (DCLK1) with an IC50 of 47 nM, and it is applicable in cancer research.

DCLK1-IN-4 (compound D2) is a potent and selective inhibitor of doublecortin-like kinase 1 (DCLK1), with an IC50 of 70 nM. It is applicable to cancer research.

DCLK1-IN-6 (Compound 12n) is an inhibitor of doublecortin-like kinase 1 (DCLK1) with an IC50 value of 58 nM. It effectively suppresses DCLK1 enzyme activity and the inflammatory pathways it mediates. This compound exhibits noteworthy anti-inflammatory properties, significantly alleviating symptoms in acute lung injury (ALI) and sepsis mouse models. DCLK1-IN-6 is useful in research on acute inflammatory diseases.

DCLK1-IN-2 (Compound I-5) is a potent inhibitor of DCLK1, exhibiting an IC50 of 171.3 nM, and demonstrates significant antiproliferative effects on SW1990 cell lines with an IC50 of 0.6 μM, as well as in vivo antitumor potency [1].

DCLK1-IN-1 is a selective, in vivo compatible chemical probe of the kinase domain of doublecortin-like kinase 1 (DCLK1) and a highly selective DCLK1/2 inhibitor with IC50 values ​​of 9.5/57.2 nM (DCLK1) and 31/103 nM (DCLK2) by binding and kinase assays, respectively. It has low toxicity and is used to study DCLK1 biology and determine its role in cancer.

DCLK1-IN-5 (Compound a24), with an IC 50 of 179.7 nM, acts as a DCLK1 inhibitor. It mitigates lipopolysaccharide-induced inflammation by blocking DCLK1-mediated IKKβ phosphorylation. Additionally, DCLK1-IN-5 offers protection to mice from lung injuries and sepsis caused by inflammation [1].

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.