| 3F8GSK-3β inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
3F8 Dilution Calculator
calculate
3F8 Molarity Calculator
calculate
| Cas No. | 159109-11-2 | SDF | Download 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 |
| Physical Appearance | Yellow solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
