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BRD0705 GSK-3 inhibitor

Name: BRD0705
Brand: Selleck Chemicals
SKU: S9638
Rating: 5 (1 reviews)

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 leukaemia (AML).

Chemical Structure

Molecular Weight: 321.42

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.96

Related Targets	PI3K Akt mTOR ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other GSK-3 Inhibitors	CHIR-99021 (Laduviglusib) Laduviglusib (CHIR-99021) Hydrochloride SB216763 CHIR-98014 TWS119 GSK-3 Inhibitor IX (BIO) LY2090314 Tideglusib SB415286 AR-A014418

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	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (10.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.530mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	GSK3α (Cell-free assay) 66 nM GSK3β (Cell-free assay) 515 nM(Kd) GSK3α (Cell-free assay) 4.8 μM(Kd)
In vitro	BRD0705 inhibits kinase function and does not stabilise 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 haematopoietic cells.
In vivo	This compound impairs leukaemia initiation and prolongs survival in AML mouse models.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29515000/

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