BRD0705

Catalog No.S9638

For research use only.

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

CAS No. 2056261-41-5

Purity & Quality Control

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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

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]

In vivo

BRD0705 impairs leukemia initiation and prolongs survival in AML mouse models.[1]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: 8-week-old male NSG mice
  • Dosages: 15 mg/kg, 30 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 64 mg/mL
(199.11 mM)
Water Insoluble
Ethanol '''64 mg/mL

Chemical Information

Molecular Weight 321.42
Formula
C20H23N3O
CAS No. 2056261-41-5
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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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

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