gsk-3β inhibitor 2

GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) is a BBB-crossing and selective inhibitor of GSK-3β (IC50 = 1.1 nM). GSK-3β inhibitor 2 can be used in studies about Alzheimer's disease.

GSK-3β inhibitor23 (Compound 11726169) is an inhibitor of glycogen synthase kinase 3 (GSK-3), effectively inhibiting GSK-3β and GSK-3α with IC50 values of 12.1 nM and 18.8 nM, respectively. It demonstrates antiviral activity against HIV1 and exhibits good metabolic stability in mouse and human liver microsomes and plasma, although it has poor permeability in Caco-2 cells, indicating potentially low oral bioavailability.

GSK-3β inhibitor24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. It increases GSK-3β phosphorylation at the Ser9 site in a dose-dependent manner and inhibits tau protein hyperphosphorylation by reducing the abundance of p-tau-Ser396. The compound upregulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2), demonstrating significant anti-Alzheimer's disease (AD) activity.

GSK-3β inhibitor20 (compound 3A) is an effective inhibitor of GSK-3β, exhibiting an IC50 value of 74.4 nM.

GSK-3β inhibitor26 (Compound D14) is a GSK-3β inhibitor with an IC50 of 18.23 μM. This compound is applicable in research related to cancer, inflammation, and neurodegenerative diseases.

GSK-3β Inhibitor21 (compound 44) is an ATP-competitive inhibitor of GSK-3β with an IC50 value of 6.06 µM, characterized by its ability to inhibit tau phosphorylation and prevent amyloid protein aggregation. This compound is utilized in the research of Alzheimer's disease.

GSK-3β inhibitor22 (compound 20o) is a GSK-3β inhibitor with an IC50 of 3.1 nM, showing potential for Alzheimer's disease research.

GSK-3β inhibitor25 (Compound 6h) exhibits weak inhibitory activity against GSK-3β with an IC50 greater than 100 μM.

GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.

GSK-3 inhibitor6 (2) is a GSK-3 inhibitor that exhibits CNS permeability, displaying IC50 values of 29 nM for GSK-3α and 24 nM for GSK-3β.

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.

COB-187 is an effective, ATP-competitive, selective inhibitor of GSK-3β. It inhibits GSK-3 through a reversible, cysteine (Cys)-199 dependent mechanism. Additionally, COB-187 suppresses the production of cytokines induced by LPS and the production of CXCL10 triggered by the SARS-CoV-2 spike protein.

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.

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.

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.

Alsterpaullone, 2-Cyanoethyl is a selective dual inhibitor of Cdk1 cyclin B and GSK-3β.

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.

CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.

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.

TFGF-18 is a GSK-3β inhibitor with an IC50 of 0.59 μM. It suppresses microglial activation and the release of pro-inflammatory mediators induced by LPS by inhibiting GSK-3β and downstream p65 NF-κB signaling. TFGF-18 also prevents neuronal apoptosis and oxidative stress, reduces the expression of Bax, caspase-3, and cleaved-caspase-3, while increasing Bcl-2 expression. It offers neuroprotection by inhibiting neuroinflammation and alleviating cognitive impairment.