CLK1

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).

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

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

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.

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.

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.

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

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.

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].

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.

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.

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

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).

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

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.

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).

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.

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.

MDK6204 is a selective inhibitor of CLK1 and CLK2.