>>Signaling Pathways>> PI3K/Akt/mTOR Signaling>> GSK-3>>3F8

3F8

Catalog No.GC14306

3F8은 GSK3 관련 질병에 대한 새로운 시약 및 잠재적 치료 후보로 유용할 수 있는 강력하고 선택적인 GSK-3β 억제제입니다.

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3F8 Chemical Structure

Cas No.: 159109-11-2

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10mg
US$140.00
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50mg
US$536.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 34 and 304 nM in the presence of 10 and 100 μM ATP, respectively.

3F8 is a potent and selective GSK-3β (Glycogen Synthase Kinase 3) inhibitor

GSK3 was identified as a serine/threonine protein kinase for the first time in the late 1970s and is highly conserved in all animals examined. GSK3 can regulate cell differentiation and apoptosis, and is an important component of the canonical Wnt pathway as well as the hedgehog pathway

In vitro: 3F8 specifically abolishes eye and forebrain formation in zebrafish embryos with the similar as a typical Wnt overexpression phenotype. Cell reporter assays, chemical informatics analysis and in vitro kinase experiments exhibited that 3F8 is a selective GSK3 inhibitor with more potent than SB216763 (a commonly used GSK3 inhibitor). Together, 3F8 and its derivatives could be useful as new agents and potential therapeutic candidates for GSK3 related diseases [1].

The interaction of 3F8 with its binding site were studied. To this end, first computational analysis conducted, and the results suggested that maleimide moiety of 3F8 might interact with the ATP binding site of GSK-3β, and the N-4 and C-5 positions were solvent-exposed, indicating the less key role of this region to the binding affinity. [2].

In vivo: The lowest ratio (CE/IC50 = 221) of 3F8 implied that 3F8 was more efficient in vivo, likely according to better absorption and/or stability [1]. By injection of a sub-lethal amount of morpholino antisense oligonucleotides, individual knockdown of gsk3a and gsk3b translations in zebrafish caused cardiac defect [1].

Clinical trial: Clinical study has been conducted.

References:
[1].  Zhong H, Zou H, Semenov MV, Moshinsky D, He X, Huang H, Li S, Quan J, Yang Z, Lin S. Characterization and development of novel small-molecules inhibiting GSK3 and activating Wnt signaling. Mol Biosyst. 2009 Nov;5(11):1356-60.
[2].  Zou H, Zhou L, Li Y, Cui Y, Zhong H, Pan Z, Yang Z, Quan J. Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode. J Med Chem. 2010 Feb 11;53(3):994-1003.

Chemical Properties

Cas No. 159109-11-2 SDF
Chemical Name 5-ethyl-1-hydroxy-7,8-dimethoxy-3H-pyrrolo[3,4-c]isoquinolin-3-one
Canonical SMILES CCC1=NC2=C(C(O)=NC2=O)C3=CC(OC)=C(OC)C=C31
Formula C15H14N2O4 M.Wt 286.28
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.4931 mL 17.4654 mL 34.9308 mL
5 mM 0.6986 mL 3.4931 mL 6.9862 mL
10 mM 0.3493 mL 1.7465 mL 3.4931 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

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