sk3

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

CyPPA, a subtype-selective positive modulator of SK channels, decreased spontaneous firing rate, increased the duration of the apamin-sensitive afterhyperpolarization.

SK3 Channel-IN-1 (compound 7a) is a potent and selective SK3 channel modulator that effectively inhibits breast cancer MDA-MB-435 cell migration with low cytotoxicity in other cell lines, and it modulates ion channel activity in cancer cells [1].

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).

GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases.

GSK3-IN-4 is a GSK-3 inhibitor with IC50 of 0.101-1 μM of GSK-3α and GSK-3β in Calipe Assay.

GSK3-IN-2 is a potent GSK3 inhibitor for the treatment of diabetes and neurodegenerative diseases.

GSK3004774 is a nonabsorbable agonist of CaSR (pEC50: 7.3, 6.6, and 6.5 for human, mouse, and rat CaSR). GSK3004774 shows an EC50 of 50 nM for human CaSR.

GSK3532795 is a potent, orally active, second-generation HIV-1 maturation inhibitor (EC50s: 10.2, 1.9, 2.7, and 13 nM for HIV-1 WT(human serum), HIV-1 WT, HIV-1 V370A, and HIV-1 ΔV370).

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.

SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity.

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.

GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.

GSK3395879 is a selective, orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) with an IC50 of 1 nM for hTRPV4.

GSK376501A is a selective and effective modulator of peroxisome proliferator-activated receptor γ (PPARγ) for the study of type 2 diabetes.

GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma.

GSK3787 is a specific and irreversible PPARδ inhibitor(pIC50= 6.6).

GSK3335103 is a non-peptide, orally active inhibitor of αvβ6 integrin (pIC50=8), employed in the study of pulmonary fibrosis.

GSK3β-IN-1 (compound 1) is an inhibitor of glycogen synthase kinase-3β (GSK-3β) with an IC50 value of 65 nM, and it is utilized in Alzheimer's disease research.

CDKL5 GSK3-IN-1 (Compound 2) acts as a potent and selective chemical probe for CDKL5 and GSK3. It effectively inhibits CDKL5 and GSK3α β with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α in NanoBRET assays. This compound is useful in the study of central nervous system disorders.

GSK3β-IN-2 (Compound S01) is an inhibitor of GSK3β with an IC50 of 0.35 nM. It activates the Wnt β-catenin signaling pathway, promoting neurogenesis and neurite outgrowth. GSK3β-IN-2 reduces tau protein phosphorylation induced by Aβ at the Ser396 site, thereby decreasing neurofibrillary tangles. Furthermore, GSK3β-IN-2 improves Alzheimer's disease symptoms in a zebrafish model.

GSK3-IN-9 (0713) is a selective inhibitor of glycogen synthase kinase 3 (GSK3). It holds potential for research into fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood epilepsy, intellectual disabilities, diabetes, acute myeloid leukemia (AML), autism, and mental disorders.