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GSK-3β inhibitor 3

Catalog No. T35554   CAS 1448990-73-5

GSK-3β inhibitor 3 is a covalent inhibitor (IC50: 6.6 μM) of glycogen synthase kinase 3β (GSK-3β) that is potent, selective, and irreversible.GSK-3β inhibitor 3 can be used to study acute promyelocytic leukemia.

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GSK-3β inhibitor 3 Chemical Structure
GSK-3β inhibitor 3, CAS 1448990-73-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 98.00
5 mg In stock $ 247.00
10 mg In stock $ 393.00
25 mg In stock $ 659.00
50 mg In stock $ 939.00
100 mg In stock $ 1,270.00
500 mg In stock $ 2,550.00
1 mL * 10 mM (in DMSO) In stock $ 272.00
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Purity: 97.53%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK-3β inhibitor 3 is a covalent inhibitor (IC50: 6.6 μM) of glycogen synthase kinase 3β (GSK-3β) that is potent, selective, and irreversible.GSK-3β inhibitor 3 can be used to study acute promyelocytic leukemia.
Targets&IC50 GSK-3β:6.6 μM (IC50)
In vitro GSK-3β inhibitor 3 (compound 4-3) (6.25-100 μM; 24-48 h) dose-dependently inhibited the cell viability, with IC50s of 19.56 μM and 26.42 μM in NB4 and NB4-R1 cells at 24 h, respectively. GSK-3β inhibitor 3 (12.5-100 μM; 24 h) significantly increases the percentage of apoptosis in a dose-dependent pattern in NB4 and NB4-R1 cells.[1]
GSK-3β inhibitor 3 (100 μM) inhibits GSK-3α activity by 87.3%.[1]
In vivo GSK-3β inhibitor 3 (compound 4-3) (15 mg/kg; a single i.p.; Balb/c female nude mice) shows T1/2 value 14.2 h, AUC values (AUClast=3503.42 ng/mL•h), and maximum concentration (Cmax=515 ng/mL) in mice.[1]
GSK-3β inhibitor 3 (15 mg/kg/d; i.p. for 2 weeks; Balb/c female nude mice) inhibits tumor growth of mice by 75.97% relative to vehicle control.[1]
Molecular Weight 327.37
Formula C18H14FNO2S
CAS No. 1448990-73-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225.0 mg/mL (687.3 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Zhang P, et al. Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. J Med Chem. 2021;64(11):7341-7358.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

GSK-3β inhibitor 3 1448990-73-5 Apoptosis PI3K/Akt/mTOR signaling Stem Cells GSK-3 GSK-3beta inhibitor 3 GSK3β inhibitor 3 GSK 3β inhibitor 3 GSK-3b inhibitor 3 inhibitor inhibit

 

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