GSK 3β inhibitor 1

GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.

(E Z)-GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor demonstrating high antidiabetic efficacy.

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

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

GSK-3β inhibitor 11 (compound 21) is a potent glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 10.02 μM, demonstrating potential utility in neurodegenerative disease research [1].

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

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50 values of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively, and exhibits neuroprotective effects [1].

hAChE hBuChE GSK-3β-IN-1 (Compound 6c) is a multi-target compound designed for Alzheimer's treatment capable of crossing the blood-brain barrier. It inhibits hAChE with an IC50 of 28.88 nM, hBuChE with an IC50 of 131.90 nM, and GSK-3β with an IC50 of 51.42 nM. Additionally, it acts as an inhibitor of tau protein and Aβ protein aggregation.

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.

GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC 50 of 35 nM. GSK-3β inhibitor 9 exhibits good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 is able to be used for the research of Alzheimer's disease [1].

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

18BIOder is a neuroprotective inhibitor of GSK-3β, highly selectively inhibiting HIV-1. It is the second generation derivative of 6BIO.

SAR502250 is a potent, selective, ATP-competitive, orally active, and brain-penetrant GSK3 inhibitor with a human GSK-3β IC50 value of 12 nM, exhibiting antidepressant-like activity and being researched for potential application in Alzheimer's disease (AD) treatment.

ZDWX-25 is a highly potent dual inhibitor of GSK-3β and DYRK1A, exhibiting significant cytotoxic activities towards SH-SY5Y and HL-7702 cells, and an IC 50 value of 71 nM for GSK-3β [1]. ZDWX-25 can be used for Alzheimer's disease research.

GSK-3β inhibitor 6 is a highly potent inhibitor of GSK-3β with an IC50 value of 24.4 μM, significantly enhancing hepatocyte glucose uptake (38%). This compound holds great potential for studying diseases such as diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder [1].

TDZD-8 (NP 01139) is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.

1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1 cyclin B and CDK5 p25.

AChE GSK-3β-IN-1 is a potent dual AChE GSK-3β inhibitor that crosses the blood-brain barrier and acts on hAChE (IC50: 1.2 nM), hBChE (IC50: 149.8 nM) and hGSK-3β (IC50: 22.4 nM). AChE GSK-3β-IN-1 is able to occupy the ATP binding site of DYRK1A. aChE GSK-3β-IN-1 exhibits high kinase selectivity for the CMGC kinase family. aChE GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. aChE GSK-3β-IN-1 can be used to study Alzheimer's disease.

Hymenialdisine Analogue #1 is the indole derivative of Hymenialdisine, a potent inhibitor of a variety of kinases including MEK-1, GSK-3Β, and CKI. It also exhibits inhibition of the G2 cell cycle checkpoint at the micromolar concentrations.

RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM), cyclin D1-CDK4 (IC50 = 4 nM), cyclin E-CDK3 (IC50 = 5 nM), and p35-CDK5 (IC50 = 5 nM). Additionally, it inhibits other kinases such as GSK-3β (IC50 = 3 nM), TAK1 (IC50 = 5 nM), Jak2 (IC50 = 50 nM), and MEK1 (IC50 = 54 nM), showcasing its versatile inhibitory potential.

GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-induced iNOS expression, demonstrating neuroprotective properties against Aβ 1-42-induced neurotoxicity and indicating potential utility in Alzheimer's disease (AD) research [1].

FSC231 is a protein kinase Cα-interacting protein 1 (PICK1) inhibitor with analgesic activity, alleviating paclitaxel-induced neuropathic pain by inhibiting PICK1 and modulating related factors, activating GSK-3β and ERK1 2.

GSK-3β Inhibitor 17 (compound 5 n) reduces the expression of p-p65 and KIM-1 proteins in a dose-dependent manner (16, 32, 64 µM) induced by cisplatin. Additionally, at a concentration of 32 µM, it decreases the levels of TNF-α, IL-1β, IL-6, and MCP-1 mRNA in an acute kidney injury (AKI) model of HK-2 cells triggered by cisplatin.

GSK3-IN-1 is a GSK3B-glycogen synthase kinase-3 beta inhibitor.