BAM7

製品コードS7105 バッチS710501

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₁₉N₅O₂S

分子量

405.47

CAS No.

331244-89-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

2 mg/mL (4.93 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.100mg/ml (0.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.100mg/ml (0.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 2 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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	BAM 7は、プロアポトーシス性Baxの直接的かつ選択的な活性化因子であり、EC50は3.3 μMです。
in vitro	BAM7 directly binds the previously uncharacterized BH3-binding groove at the N-terminal face of BAX. This compound is selective for the BH3-binding groove at the N-terminal face of BAX. It directly interacts with BAX at the very surface used by the BIM BH3 helix to trigger BAX activation. This chemical results in functional BAX activation. It triggers the conversion of BAX from monomer to oligomer in a dose- and time-responsive manner, the kinetics of which approach saturation at a 1:8 dose ratio of BAX:BAM7. This compound triggers in vitro BAX oligomerization, BAX-mediated pore formation and BAX-dependent cell death. It selectively induces BAX-mediated apoptosis by triggering the hallmark features of intracellular BAX activation. This chemical only kills the cell line that contains BAX, eliciting the biochemical and morphologic features of BAX-mediated apoptosis.
特徴	Does not interact with the BH3-binding pocket of antiapoptotic proteins or proapoptotic BAK and induces cell death in a BAX-dependent fashion.

プロトコル(参考用のみ)

キナーゼアッセイ	Fluorescence polarization binding assays
キナーゼアッセイ	Direct binding curves are first generated by incubating FITC-BIM SAHB (50 nM) with serial dilutions of fulllength BAX, BCL-XLΔC, MCL-1ΔNΔC, BFL-1/A1ΔC or BAKΔC and fluorescence polarization measured at 20 minutes on a SpectraMax M5 microplate reader. For competition assays, a serial dilution of this compound or acetylated BIM SAHB (Ac-BIM SAHB) is combined with FITC-BIM SAHB (50 nM), followed by the addition of recombinant protein at ~EC75 concentration, as determined by the direct binding assay (BAX, BAKΔC: 500 nM; BCL-XLΔC, MCL-1ΔNΔC, BFL-1/A1ΔC: 200 nM). Fluorescence polarization is measured at 20 minutes and IC50 values calculated by nonlinear regression analysis of competitive binding curves using Prism software.
細胞アッセイ	細胞株	MEFs
	濃度	~15 μM
	反応時間	24 h
	実験の流れ	MEFs (2.5 × 10³ cells per well) are seeded in 96-well opaque plates for 18-24 h and then incubated with serial dilutions of BAM7, ANA-BAM16 or vehicle (0.15% (v/v) DMSO) in DMEM at 37 °C in a final volume of 100 μL. Cell viability is assayed at 24 h by addition of CellTiter-Glo reagent according to the manufacturer’s protocol, and luminescence is measured using a SpectraMax M5 microplate reader. Viability assays are performed in at least triplicate, and the data are normalized to vehicle-treated control wells.

参考

https://pubmed.ncbi.nlm.nih.gov/22634637/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Small-molecule allosteric inhibitors of BAX. [ Nat Chem Biol, 2019, 15(4):322-330]	PubMed: 30718816
Survival of midbrain dopamine neurons depends on the Bcl2 factor Mcl1 [ Cell Death Discov, 2018, 4:107]	PubMed: 30479840
Drug manipulation of pro-and anti-apoptotic Bcl-2 proteins in the regulation of Parkin-mediated mitophagy in human breast cancer cells [ Baltimore, Maryland , 2018, ]	PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。