GSK-3β Inhibitor

GSK-3β Inhibitors (140):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-172198

GSK3-IN-10	Inhibitor
GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC₅₀ of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress.

HY-181811

PJ17	Inhibitor
PJ17 is a potent dual-target inhibitor of AChE and GSK-3β, with IC₅₀ values of 8.84 μM and 4.19 μM, respectively. PJ17 shows no significant neurotoxic effect in primary cerebellar granule neuron cultures. PJ17 serves as a template for the design of multitarget drugs. PJ17 can be used for the research of Alzheimer's disease.

HY-143260

GSK-3β inhibitor 6	Inhibitor
GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC₅₀ value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.

HY-W098905

GSK3β-IN-3	Inhibitor
GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC₅₀ = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tau protein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD).

HY-151878

CDK7-IN-20	Inhibitor
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC₅₀ value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.

HY-126125

CHIR-98023	Inhibitor
CHIR-98023 is a potent, selective and reversible inhibitor of GSK3, with IC₅₀s of 10 nM and 6.7 nM for GSK3α and GSK3β, respectively. CHIR-98023 can improve insulin action and glucose metabolism.

HY-100006B

MRT68921 hydrochloride	Inhibitor
MRT68921 hydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 hydrochloride inhibits ULK1 and ULK2 with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. MRT68921 hydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 hydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 hydrochloride can be used for the research of cancer, such as breast cancer.

HY-161751

MJ34	Inhibitor
MJ34 is a potent inhibitor of GSK-3β and GSK-3α, with the IC₅₀s of 15.4 nM and 31.5 nM, respectively. MJ34 plays an important role in cancer research

HY-179723

GSK3β-IN-4	Inhibitor
GSK3β-IN-4 is a selective, potent, orally active and brain-penetrant ATP-competitive GSK3β inhibitor with an IC₅₀ of 0.37 nM. GSK3β-IN-4 shows an IC₅₀ of 2.75 nM and SI of 7.4 for GSK3α. GSK3β-IN-4 reduces tau phosphorylation at Ser396 by inhibiting GSK3β and imoroves cognitive deficits in Alzheimer's disease models. GSK3β-IN-4 can be used for the research of Alzheimer's disease.

HY-178142

Multi-kinase-IN-7	Inhibitor
Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum antiproliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

HY-143261

GSK-3β inhibitor 7	Inhibitor
GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC₅₀ value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.

HY-107529

TC-G 24	Inhibitor
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC₅₀ of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases.

HY-163748

GSK-3β inhibitor 17	Inhibitor
GSK-3β inhibitor 17 (compound 5 n) is a potent GSK-3β inhibitor. GSK-3β inhibitor 17 decreases cisplatin (HY-17394) induced p-p65, KIM-1 protein and mRNA expression. GSK-3β inhibitor 17 decreases cisplatin induced TNF-α, IL-1β, IL-6 and MCP-1 mRNA expression. GSK-3β inhibitor 17 shows anti-inflammation effect and has the potential for the research of acute kidney injury.

HY-181248

BChE-IN-49	Inhibitor
BChE-IN-49 is an orally active BChE inhibitor with IC₅₀ values of 0.73 μM and 6.43 μM against BChE and AChE, respectively. BChE-IN-49 reduces AChE levels to inhibit the degradation of acetylcholine. By inhibiting GSK-3β, BChE-IN-49 potently activates the Wnt/β-catenin signaling pathway, exerting potent anti-Aβ, antioxidant, anti-neuroinflammatory and anti-apoptotic effects. BChE-IN-49 can be used in research related to Alzheimer's disease.

HY-181160

JNK3/Wnt/β-catenin modulator-1	Inhibitor
JNK3/Wnt/β-catenin modulator-1 is a brain-penetrant JNK3 inhibitor and Wnt/β-catenin activator. JNK3/Wnt/β-catenin modulator-1 decreases Aβ_1-42 production and reduced ROS generation. JNK3/Wnt/β-catenin modulator-1 inhibits the activation of JNK and Puma, promotes Beclin-1 expression, reduces GSK-3β and BACE1 expression and activates Wnt/β-catenin signaling. JNK3/Wnt/β-catenin modulator-1 improves cognitive and memory performance, attenuates histopathological brain damage, preserves structure of hippocampal pyramidal cells and cerebral cortical neurons. JNK3/Wnt/β-catenin modulator-1 can be used for the research of Alzheimer's disease.

HY-151962

JNK3 inhibitor-5	Inhibitor
JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC₅₀ of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable.

HY-174272

GSK-3β inhibitor 27	Inhibitor
GSK-3β inhibitor 27 (Compound 1c) is a reversible and competitive GSK-3β inhibitor with an IC₅₀ value of 2.2 μM. GSK-3β inhibitor 27 inhibits tau hyperphosphorylation, reduces Aβ protein aggregation and possesses metal chelation and neuroprotective potential. GSK-3β inhibitor 27 is promising for research of neurodegenerative diseases (such as Alzheimer’s disease).

HY-180938

Fyn-IN-1	Inhibitor
Fyn-IN-1 (Compound 43) is a selective, blood-brain barrier permeable Fyn and GSK-3β inhibitor with IC₅₀ values of 0.044 μM and 0.61 μM, respectively. Fyn-IN-1 significantly downregulates the pro-inflammatory enzyme iNOS. Fyn-IN-1 can be used in the research of neurodegenerative diseases.

HY-W657887

GSK-3β/G9a-IN-1	Inhibitor
GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC₅₀: 1.1 μM) and GSK-3β (ATP competitive, IC₅₀: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.

HY-172586

GSK-3α/β-IN-1	Inhibitor
GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC₅₀s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC₅₀ of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC₅₀: 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM.

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