Home PI3K/Akt/mTOR GSK-3 inhibitor BRD0705 For research use only.

BRD0705

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. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).

BRD0705 Chemical Structure

BRD0705 Chemical Structure

CAS No. 2056261-41-5

Purity & Quality Control

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

BRD0705 Related Products

Signaling Pathway

GSK-3 Signaling Pathways

GSK-3 Signaling Pathway

Biological Activity

Description 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. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).
Targets
GSK3α [1]
(Cell-free assay)		 GSK3β [1]
(Cell-free assay)		 GSK3α [1]
(Cell-free assay)
66 nM 515 nM(Kd) 4.8 μM(Kd)
In vitro
In vitro

BRD0705 inhibits kinase function and does not stabilize β-catenin, mitigating potential neoplastic concerns. BRD0705 induces myeloid differentiation and impairs colony formation in AML cells while no effect is observed on normal hematopoietic cells.[1]
Cell Research Cell lines HEK 293T, HL-60, U937, TF-1, NB-4, MV4–11, MOLM-13, Mononuclear cells
Concentrations 20 μM
Incubation Time 24 hours
Method

After 24 hours of treatment with DMSO or BRD0705 at 20 μM, 30,000 to 50,000 cells are washed in PBS/2%FBS and then cytospun onto poly-L-Lysine coated slides (EMS). Cells are fixed in 4% paraformaldehyde (EMS) for 20 minutes, permeabilized in 0.2% Triton X-100 (RPI) for 30 minutes at 4°C, blocked in 1% BSA/0.05% triton for 1 hour at room temperature and then incubated for 1 hour at room temperature with primary anti-β-catenin (1/500) and then secondary antibody. Three 5 minute washes are performed after each antibody incubation. Slides are mounted with Prolong (R) Gold Antifade with DAPI and imaged with Yokogawa Spinning Disk Confocal / TIRF system. Representative images of three independent experiments are analyzed with Image-J software.
In Vivo
In vivo

BRD0705 impairs leukemia initiation and prolongs survival in AML mouse models.[1]
Animal Research Animal Models 8-week-old male NSG mice
Dosages 15 mg/kg, 30 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 321.42 Formula
C20H23N3O
CAS No. 2056261-41-5 SDF --
Smiles CCC1(C2=CC=CC=C2)C3=CNNC3=NC4=C1C(=O)CC(C)(C)C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 64 mg/mL ( (199.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy BRD0705 | BRD0705 supplier | purchase BRD0705 | BRD0705 cost | BRD0705 manufacturer | order BRD0705 | BRD0705 distributor