clk 1

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).

CLK1/2-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.

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.

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

MDK6204 is a selective inhibitor of CLK1 and CLK2.

SGC-CLK-1 is a potent and selective inhibitor of Cdc2-like kinases CLK1, CLK2, and CLK4. It effectively inhibits the growth of melanoma and glioblastoma cells.

CLK2/3-IN-1 (Compound 7c) is an orally active inhibitor of CLK2/3, with EC50 values of 5.07 nM and 30.03 nM, respectively. Its inhibitory action is facilitated by hydrogen bonding with Lys193 and Lys186 residues of CLK2/3. This compound effectively inhibits the proliferation of SW480 tumor cells with an IC50 of 163 nM and is applicable for research into CLK-related cancer diseases.

LRRK2 inhibitor 1 is a selective and potent LRRK2 inhibitor with an IC50 of 13 nM.LRRK2 inhibitor 1 inhibits DCLK1 kinase with an IC50 value of 2.61 nM.

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.

Leucettine L41 (LeucettineL41) is a selective DYRK1A inhibitor that inhibits DYRK2, CLK1, and CLK3, inducing autophagy linked to CLK inhibition. It is used to study Alzheimer's disease and memory deficits.

Leucettinib-92 is a small-molecule inhibitor of the DYRK and CLK kinase families that exhibits differential inhibitory activity across multiple kinases, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3, supporting its use in kinase signaling and regulatory mechanism research.

(E/Z)-TG003 is a potent and ATP-competitive inhibitor of Cdc2-like kinase (Clk).

MU1210 (compound 12f) acts as an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 with IC50 values of 8, 20, and 12 nM, respectively, and exhibits IC50 values of 187 and 1309 nM for HIPK1 and DYRK2. Additionally, MU1210 demonstrates favorable pharmacokinetic properties in mice (10 mg/kg, intraperitoneal injection: Cmax=1.24 μM, T1/2=58 minutes; no acute toxicity observed).