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BOC Sciences
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Product Name:GSK-3β inhibitor 3
CAS:1448990-73-5
Purity:>=95% Remarks:Reach out to us for more information about custom solutions.
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| Company Name: |
Bide Pharmatech Ltd.
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400-1647117 13681763483 |
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product02@bidepharm.com |
| Products Intro: |
Product Name:5-Acryloyl-2-(4-fluorophenyl)-2,3-dihydrobenzo[b][1,4]thiazepin-4(5H)-one
CAS:1448990-73-5
Purity:98% Package:25mg;50mg;100mg Remarks:BD01479436
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1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)- manufacturers
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| | 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)- Basic information |
| Product Name: | 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)- | | Synonyms: | 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)-;GSK-3β inhibitor 3;GSK3β inhibitor 3,GSK 3β inhibitor 3;5-Acryloyl-2-(4-fluorophenyl)-2,3-dihydrobenzo[b][1,4]thiazepin-4(5H)-one;GSK-3β inhibitor 3, 10 mM in DMSO | | CAS: | 1448990-73-5 | | MF: | C18H14FNO2S | | MW: | 327.37 | | EINECS: | | | Product Categories: | | | Mol File: | 1448990-73-5.mol |  |
| | 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)- Chemical Properties |
| Boiling point | 489.0±45.0 °C(Predicted) | | density | 1.297±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (763.66 mM; Need ultrasonic) | | form | Solid | | pka | -0.61±0.40(Predicted) | | color | White to off-white |
| | 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)- Usage And Synthesis |
| Uses | 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[1]. | | Biological Activity | 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[1].
GSK-3β inhibitor 3 (compound 4-3) (100 μM) inhibits GSK-3α activity by 87.3%[1].GSK-3β inhibitor 3 (6.25-100 μM; 24-48 h) dose-dependently inhibits the growth of NB4 and NB4-R1 cells[1].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 (compound 4-3) (15 mg/kg/d; i.p. for 2 weeks) inhibits tumor growth of mice by 75.97% relative to vehicle control[1].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/mLh), and maximum concentration (Cmax=515 ng/mL) in mice[1]. | | 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[1].
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/mLh), and maximum concentration (Cmax=515 ng/mL) in mice[1]. | Animal Model: | Balb/c female nude mice were injected leukemia cells[1] | | Dosage: | 15 mg/kg/d | | Administration: | I.p. for 2 weeks | | Result: | Inhibited localized growth in NB4 cells.
Had mild weight loss compared with control. |
| Animal Model: | Male ICR mice (30 g)[1] | | Dosage: | 15 mg/kg (Pharmacokinetic Analysis) | | Administration: | A single i.p. | | Result: | T1/2=14.2 h; AUClast=3503.42 ng/mLh; Cmax=515 ng/mL. |
| | IC 50 | GSK-3β: 6.6 μM (IC50) | | References | [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 May 24. |
| | 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)- Preparation Products And Raw materials |
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