clk

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.

Cirtuvivint (SM08502) is a potent, orally active CDC-like kinase (CLK) inhibitor useful for the study of arthritis.

ML 315 is a selective Clk and DYRK inhibitor with potential anticancer activity for the study of neurological disorders.

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).

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

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.

CLK1/2-IN-1 is a CLK1 and CLK2 inhibitor and it also inhibits SRPK1 and SRPK2.

CLK-IN-T3N, the negative control of CLK-IN-T3 , is a chemical probe for CDC-like kinase (CLK) .

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).

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.

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.

CLK8 is a selective CLOCK inhibitor that binds to and interferes with CLOCK activity, disrupts the interaction between CLOCK and BMAL1, and modulates circadian rhythm amplitude.CLK8 can be used to study circadian rhythm-related disorders.

PfCLK3-IN-1 (Compound 4) serves as a covalent inhibitor of the malaria parasite CLK3 (Pf CLK3) under alkaline conditions, with a pEC50 of 7.1. It inhibits the maturation of gametocytes during the sexual stage of the parasite, thereby hindering transmission. Additionally, PfCLK3-IN-1 effectively suppresses the Dd2-B2 clone of the malaria parasite, exhibiting an IC50 of 239.5 nM.

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].

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.

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

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.