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.

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.

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 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-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.

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

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-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].

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.

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).

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].

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.

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).

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).

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.