BDA-366

Catalog No.S7849

For research use only.

BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).

BDA-366 Chemical Structure

CAS No. 1909226-00-1

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Biological Activity

Description BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).
Targets
Bcl2-BH4 [2]
(Cell-free assay)
3.3 nM(Ki)
In vitro

BDA-366 induces robust apoptosis in MM(Multiple myeloma) cell lines and primary MM cells by inducing BCL2 conformational change. BDA-366 induces a conformational change in the BCL2 molecule that converts it to a death protein, and inhibits lung cancer growth in vitro and in vivo[1]. BDA-366 did not bind to other Bcl2 family members, including Bcl-XL, Mcl-1, or Bfl-1/A1, indicating the specificity of its Bcl2 binding. BDA-366 induces apoptotic cell death in a Bax-dependent manner and induces calcium (Ca2+) release via inhibition of Bcl2/IP3R interaction[2].

In vivo Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγ null mice, without significant cytotoxic effects on normal hematopoietic cells or body weight[1]. Also, BDA-366 suppresses lung cancer growth via induction of apoptosis in animal models. The BH4 antagonist BDA-366 exhibits potent efficacy against human lung cancer in vivo without platelet reduction[2].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: human MM RPMI8226 and U266 cell lines
  • Concentrations: 0, 0.1, 0.25, 0.5 μM
  • Incubation Time: 48 h
  • Method: Human MM cell lines RPMI8226 and U266 were treated with BDA366 at increasing concentrations (0, 0.1, 0.25, 0.5μM) for 48hr. Cells were harvested, stained with Annexin V and propidium iodide (PI), and subjected to FACS analysis. Apoptotic cells were gated on the Annexin V positive population. Annexin V+PI− cells were early apoptotic cells, Annexin+PI+ cells were late apoptotic cells, and Annexin−PI+ cells were necrotic cells.
Animal Research:[1]
  • Animal Models: NSG mice
  • Dosages: 10 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 423.5
Formula

C24H29N3O4

CAS No. 1909226-00-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)CC(CNC1=C2C(=C(C=C1)NCC3CO3)C(=O)C4=CC=CC=C4C2=O)O

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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.

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