ks-i

Perfluorinated SAHA is an HDAC inhibitor for use in cancer treatment regimens, with demonstrated greater antiproliferative properties than SAHA . PFSAHA has also been shown to have higher selectivity for PA3774, an HDAC-like enzyme from P. aeruginosa, as well as other HDACs, which may prove beneficial for developing novel chemotherapeutic treatments for cancer.

KS I is a gonadotropin antagonist and is a cyclolignan isolated from extracts of Lycopus and Lithosperum after oxidation with caffeic acid.

PI5P4Ks-IN-2 is an inhibitor of the phosphatidylinositol 5-phosphate 4-kinase PI5P4Kγ. Targeting the PI5P4K isoforms, PI5P4Ks-IN-2 inhibited PI5P4Kα, PI5P4Kβ, PI5P4Kγ, and PI5P4Kγ+, with IC50 values of <4.3, <4.6, 6.2, and 0.32, respectively.

DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively.

PI5P4Ks-IN-1 (compound 7) is an active compound that interacts with PI5P4Kγ[1].

TNKS-IN-1 is a highly potent and selective inhibitor of tankyrase.

SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, functions as an inhibitor of Salt-inducible kinases (SIKs), which play a role in M1 M2 macrophage polarization linked to inflammation. By inhibiting SIK activity, this compound increases anti-inflammatory cytokine IL-10 and decreases pro-inflammatory cytokine IL-12, demonstrating significant anti-inflammatory efficacy in a DSS-induced colitis model [1].

TNKS-IN-41 highly potent and selective inhibitor of tankyrase.

DYRKs-IN-1 hydrochloride is a potent inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), with IC50 values of 5 nM for DYRK1A and 8 nM for DYRK1B, and exhibits antitumor activity.

PI5P4Ks-IN-3 (compound 30) is a covalent inhibitor of PI5P4K with inhibition constants (IC50s) of 1.34 μM for PI5P4Kα and 9.9 μM for PI5P4Kβ, but demonstrates weak cellular activity [1].

DYRKs-IN-1 has antitumor activity. DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively.

LDHA PDKs-IN-1 (compound 20e) is a highly effective dual inhibitor of PDKs and LDHA, with IC50 values of 0.8 μM and 0.15 μM, respectively. It significantly suppresses A549 cell proliferation (EC50 = 13.2 μM), reduces lactate formation, and enhances oxygen consumption, holding great promise for cancer research [1].

LDHA PDKs-IN-2 (compound 20k) is a potent dual inhibitor of LDHA and PDKs, with IC50 values of 0.7 and 1.6 μM, respectively. It increases oxygen consumption, decreases lactate formation, and shows potential for cancer research by reducing the proliferation of A549 cells with an EC50 of 15.7 μM [1].

Azimilide Dihydrochloride (NE-10064 Dihydrochloride), a novel class III antiarrhythmic agent, blocks both the slowly activating (IKs) and rapidly activating (IKr) components of the delayed rectifier potassium current