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  3. GSK-3β inhibitor 3

GSK-3β inhibitor 3 

Cat. No.: HY-141480 Purity: 98.20%
Handling Instructions

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.

For research use only. We do not sell to patients.

GSK-3β inhibitor 3 Chemical Structure

GSK-3β inhibitor 3 Chemical Structure

CAS No. : 1448990-73-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 330 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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[1].

IC50 & Target[1]

GSK-3β

6.6 μM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: NB4 and NB4-R1 cells
Concentration: 6.25, 12.5, 25, 50, 100 μM
Incubation Time: 24, 48 hours
Result: Inhibited the cell viability, with IC50s of 19.56 μM and 26.42 μM in NB4 and NB4-R1 cells at 24 h, respectively.
Had little cytotoxicity on human normal liver cells (LO2) and human umbilical vein endothelial cells (HUVECs).

Apoptosis Analysis[1]

Cell Line: NB4 and NB4-R1 cells
Concentration: 12.5, 25, 50, 100 μM
Incubation Time: 24 hours
Result: Induced cell apoptosis.
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/mL•h), and maximum concentration (Cmax=515 ng/mL) in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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/mL•h; Cmax=515 ng/mL.
Molecular Weight

327.37

Formula

C₁₈H₁₄FNO₂S

CAS No.
SMILES

FC(C=C1)=CC=C1C2CC(N(C(C=C)=O)C3=CC=CC=C3S2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (763.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0546 mL 15.2732 mL 30.5465 mL
5 mM 0.6109 mL 3.0546 mL 6.1093 mL
10 mM 0.3055 mL 1.5273 mL 3.0546 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GSK-3β inhibitor 3GSK-3ApoptosisGlycogen synthase kinase-3Glycogen synthase kinase 3GlycogenSynthaseKinaseGSK-3βacutepromyelocyticleukemiaInhibitorinhibitorinhibit

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GSK-3β inhibitor 3
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