Home PI3K/Akt/mTOR GSK-3 inhibitor BRD0705

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BRD0705 GSK-3 inhibitor

Cat.No.S9638

BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. This compound also inhibits GSK3β with IC50 of 515 nM. It can be used for acute myeloid leukemia (AML).
BRD0705 GSK-3 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 321.42

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S963801 DMSO]64 mg/mL]false]Ethanol]64 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

Chemical Information, Storage & Stability

Molecular Weight 321.42 Formula
C20H23N3O
 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2056261-41-5 -- Storage of Stock Solutions

Synonyms N/A Smiles CCC1(C2=CC=CC=C2)C3=CNNC3=NC4=C1C(=O)CC(C)(C)C4

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (199.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
GSK3α [1]
(Cell-free assay)
66 nM
GSK3β [1]
(Cell-free assay)
515 nM(Kd)
GSK3α [1]
(Cell-free assay)
4.8 μM(Kd)
In vitro

BRD0705 inhibits kinase function and does not stabilize β-catenin, mitigating potential neoplastic concerns. This compound induces myeloid differentiation and impairs colony formation in AML cells while no effect is observed on normal hematopoietic cells.[1]
In vivo

This compound impairs leukemia initiation and prolongs survival in AML mouse models.[1]
References

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