clk4

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

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

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.

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).

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.

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

DB18 serves as a potent, selective inhibitor of CDC2-like kinases (CLKs), exhibiting IC50 values between 10-30 nM for CLK1, CLK2, and CLK4. Additionally, it possesses anti-tumor activity [1].

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).

SRI-29329 is a potent, specific inhibitor of CDC-like kinase (with IC50 of 78 nM, 16 nM and 86 nM for CLK1, CLK2 and CLK4, respectively).

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

Leucettinib-21 (LCTB-21) (compound 4) serves as a selective and potent inhibitor of DYRK1A, exhibiting IC50 values of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively. This compound is applicable for the study of Down syndrome and Alzheimer's disease [1].

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].

ZJCK-6-46 (32) is a potential orally active DYRK1A inhibitor (IC50= 0.68 nM) with favorable CNC permeability. It downregulates tau phosphorylation and improves cognitive impairments by significantly reducing the expression of phosphorylated tau proteins and neuronal loss.

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.

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

Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK CLK families, 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 [1].

EHT 5372 is a potent and selective inhibitor of DYRK's family kinases. EHT 5372 shows IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.

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.

KH-CB20, an E Z mixture, is a potent and selective inhibitor of CLK1 and CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 also inhibits DYRK1A (IC50 = 57.8 nM) and CLK3 (IC50 = 488 nM).

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).