Description
GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.
Product information
CAS Number: 1448990-73-5
Molecular Weight: 327.37
Formula: C18H14FNO2S
Chemical Name: 2-(4-fluorophenyl)-5-(prop-2-enoyl)-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepin-4-one
Smiles: C=CC(=O)N1C2=CC=CC=C2SC(CC1=O)C1C=CC(F)=CC=1
InChiKey: DJUQPBPAHPCBBX-UHFFFAOYSA-N
InChi: InChI=1S/C18H14FNO2S/c1-2-17(21)20-14-5-3-4-6-15(14)23-16(11-18(20)22)12-7-9-13(19)10-8-12/h2-10,16H,1,11H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (763.66 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GSK-3β inhibitor 3 (compound 4-3) (100 μM) inhibits GSK-3α activity by 87.3%. GSK-3β inhibitor 3 (6.25-100 μM; 24-48 h) dose-dependently inhibits the growth of NB4 and NB4-R1 cells. 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.
In Vivo:
GSK-3β inhibitor 3 (compound 4-3) (15 mg/kg/d; i.p. for 2 weeks) inhibits tumor growth of mice by 75.97% relative to vehicle control. GSK-3β inhibitor 3 (15 mg/kg; a single i.p.) shows long T1/2 of 14.2 h, high AUC values (AUClast=3503.42 ng/mL•h), and maximum concentration (Cmax=515 ng/mL) in mice.
Products are for research use only. Not for human use.
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