gsk-b

GSK-B, a potent γ-secretase modulator, decreases Aβ42, increases Aβ38 with no effect on Aβ40 levels.

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.

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.

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

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).

GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.

Aloisine B (AloisineB) inhibited cyclin-dependent kinase and glycogen synthase kinase with IC50 values of 0.85 µM and 0.75 µM, respectively. Aloisine B has antiviral activity and can be used to study Alzheimer's, diabetes, HIV and Parkinson's.

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC, with potential applications in cardiac, proliferative, and neurodegenerative disease research.

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5 0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

GSK8612 is a highly selective and potent inhibitor of Tank-binding Kinase-1 (TBK1, pIC50: 6.8).

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

GSK-LSD1 dihydrochloride (GSK-LSD1 2HCl) is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD utilizing enzymes (i.e. MAO-A, LSD2, MAO-B).

Ceftriaxone Sodium is a broad-spectrum β-lactam tertiary cephalosporin antibiotic with anti-inflammatory, antitumor, antibacterial, and antioxidant activities.Ceftriaxone Sodium is a covalent GSK3β and Aurora B inhibitor used in the study of sepsis and infective endocarditis.

DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.

Uprosertib (GSK2141795) is a potent, selective Akt broad-spectrum inhibitor with IC50 values of 180 328 38 nM for Akt1 Akt2 Akt3.

Ginsenoside Rg2 (Chikusetsusaponin I) is one of the major active components of ginseng, act as an NF-κB inhibitor.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

Aloisine A is a potent and selective CDK/GSK-3 inhibitor. IC50 data of Aloisine A: Cdk1/cyclin B (IC50: 150nM), Cdk2/cyclin A (IC50: 120nM), Cdk2/cyclin E (IC50: 400nM), Cdk5/p25 (IC50: 200nM), Cdk5/p35 (IC50: 160nM), GSK-3α (IC50: 500nM), GSK-3β (IC50: 6

GSK-114, a selective inhibitor of TNNI3 Interacting Kinase (TNNI3K) with IC50 of 25 nM, shows significant bias for TNNI3K over B-Raf with IC50 of 1000 nM, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellul

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].