aladdin 阿拉丁 B413853 BDA-366 1909226-00-1 97%

中文名：BDA-366

英文名：BDA-366

纯度：≥97%

货号：B413853

Cas号：1909226-00-1

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

BDA-366 is a small-moleculeBcl2-BH4domain 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 (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. 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.

In vivo

Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγ mice, without significant cytotoxic effects on normal hematopoietic cells or body weight. 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.

Cell Research(from reference)

Cell lines：human MM RPMI8226 and U266 cell lines 

Concentrations：0, 0.1, 0.25, 0.5 μM 

Incubation Time：48 h 

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