gsk-a

GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor.

GSK-A1 is a specific inhibitor of PI4KA, also inhibited calcium-driven PRL secretion without affecting calcium signaling and Prl expression. GSK-A1 has anti-hepatitis C virus (HCV) potential.

Losmapimod (GSK-AHAB) (GW856553X; SB856553; GSK-AHAB) is a specific, potent, and orally active p38 MAPK inhibitor (pKi: 8.1/7.6 for p38α/β).

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5/P25, and CDK1/cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

GSK-3484862 is a non-covalent Dnmt1 inhibitor that induces DNA hypomethylation, offering potential therapeutic benefits against cancer.

GSK-843 (GSK'843) is a selective and potent RIP3 inhibitor with an IC50 value of 8.6 nM for the structural domain of RIP3 kinase. It has potential analgesic activity, inhibits the expression of RIP3 and NLRP3 in the SDH of CFA mice, and can be used as adjunctive therapy for treating inflammation.

GSK2593074A (GSK'074) is a programmed necrosis inhibitor that displays inhibitory effects on RIP1 and RIP3.

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor that binds to the RIP3 kinase domain (IC50: 0.9 nM) and inhibits kinase activity (IC50: 0.3 nM).

Lanopepden (GSK 1322322) is a potent peptide deformylase inhibitor effective against Staphylococcus aureus strains ATCC 29213 and ATCC 25923, and is applicable in the study of pneumonia, dermatological, and infectious diseases.

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.

3F8 is a selective GSK-3β inhibitor that can be used as a new tool and potential therapeutic candidate compound for GSK3-related diseases, and can be used in the study of neurological disorders and cancer.

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A (IC50=8.6/6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

GSK-1268997 is a PRMT5 inhibitor and can be used to study advanced solid tumors.

GSK299423 (GSK-299423) is a novel DNA rotamase inhibitor with antimicrobial activity for the study of lung infections.

H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .