5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phe

Introduction：Basic information about 5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phe, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)- Basic information

• Product Name: 5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)-
• Synonyms: 5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)-;(4S)-3-(2,2-dimethylpropyl)-4,7,7-trimethyl-4-phenyl-2,6,8,9-tetrahydropyrazolo[3,4-b]quinolin-5-one
• CAS: 2056262-07-6
• MF: C24H31N3O
• MW: 377.52
• Mol File: 2056262-07-6.mol

5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)- Chemical Properties

• Boiling point: 529.3±50.0 °C(Predicted)
• density: 1.15±0.1 g/cm3(Predicted)
• storage temp.: Store at -20°C
• solubility: DMSO : 50 mg/mL (132.44 mM; Need ultrasonic)
• form: Solid
• pka: 15.22±0.60(Predicted)
• color: Light yellow to yellow

5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)- Usage And Synthesis

Uses

BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders[1].

Biological Activity

BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders[1].BRD3731 is a GSK3β- selective inhibitor extracted from patent US20160375006A1, compound example 272[1].BRD3731 (1-10 μM; 24 hours) inhibits the phosphorylation of CRMP2 in SH-SY5Y cells[1].BRD3731 (20 μM; 24 hours) decreases β-catenin S33/37/T41 phosphorylation and induces β-catenin S675 phosphorylation in HL-60 cells[2].BRD3731 (10-20 μM; 7-10 days) impairs colony formation in TF-1 and increases colony forming ability in the MV4-11 cell line[2]

IC 50

GSK-3β: 15 nM (IC₅₀); GSK-3α: 215 nM (IC₅₀)

References

[1]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1. [2]. Wagner FF, et, al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431):eaam8460.