BAI1

製品コードS8865 バッチS886501

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₉H₂₁Br₂N₃O

分子量

467.20

CAS No.

335165-68-9

Solubility (25°C)*

体外

DMSO

18 mg/mL (38.52 mM)

Ethanol

3 mg/mL (6.42 mM)

Water

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。	0.900mg/ml (1.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 18 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。	0.900mg/ml (1.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 18 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	BAI1は、解離定数（Kd）15.0 ± 4 μMのBAXの直接アロステリック阻害剤です。
in vitro	BAX activation inhibitor 1 (BAI1) demonstrates inhibition of tBID-induced BAX-mediated membrane permeabilization in a dose dependent manner with an IC50 of 3.3 μM. This compound binds to monomeric BAX at a novel allosteric site. It is a potent inhibitor of BAX conformational activation and oligomerization in solution, not by direct competition with the activator, but rather through an allosteric mechanism that favors the inactive BAX. Moreover, this chemical inhibited BAX membrane association and translocation induced either by tBID (IC50 = 5 ± 1 μΜ) or BIM SAHB (IC50 = 2 ± 1 μΜ) in a dose dependent manner and with a similar IC50 to BAX-mediated liposomal release. It selectively inhibits BAX-dependent cell death.

製品説明

BAI1は、解離定数（Kd）15.0 ± 4 μMのBAXの直接アロステリック阻害剤です。

in vitro

BAX activation inhibitor 1 (BAI1) demonstrates inhibition of tBID-induced BAX-mediated membrane permeabilization in a dose dependent manner with an IC50 of 3.3 μM. This compound binds to monomeric BAX at a novel allosteric site. It is a potent inhibitor of BAX conformational activation and oligomerization in solution, not by direct competition with the activator, but rather through an allosteric mechanism that favors the inactive BAX. Moreover, this chemical inhibited BAX membrane association and translocation induced either by tBID (IC50 = 5 ± 1 μΜ) or BIM SAHB (IC50 = 2 ± 1 μΜ) in a dose dependent manner and with a similar IC50 to BAX-mediated liposomal release. It selectively inhibits BAX-dependent cell death.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MEFs
	濃度	0-10 μM
	反応時間	8 h
	実験の流れ	Caspase 3/7 assay of WT MEFs upon pro-apoptotic TNFα/CHX treatment in the absence or presence of co-treatment with BAI1 at indicated doses for 8 hours.

参考

https://pubmed.ncbi.nlm.nih.gov/30718816/

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：

Identification of novel small molecule chaperone activators for neurodegenerative disease treatment [ Biomed Pharmacother, 2025, 187:118049]	PubMed: 40239269
Hyperthermia and cisplatin combination therapy promotes caspase-8 accumulation and activation to enhance apoptosis and pyroptosis in cancer cells [ Int J Hyperthermia, 2024, 41(1):2325489]	PubMed: 38632954
TRIM21 inhibits irradiation-induced mitochondrial DNA release and impairs antitumour immunity in nasopharyngeal carcinoma tumour models [ Nat Commun, 2023, 14(1):865]	PubMed: 36797289
cGAS-STING activation contributes to podocyte injury in diabetic kidney disease [ iScience, 2022, 25(10):105145]	PubMed: 36176590
Targeting Myocardial Mitochondria-STING-Polyamine Axis Prevents Cardiac Hypertrophy in Chronic Kidney Disease [ JACC Basic Transl Sci, 2022, 7(8):820-840]	PubMed: 36061341
A kinetic fluorescence polarization ligand assay for monitoring BAX early activation [ Cell Rep Methods, 2022, 2(3)100174]	PubMed: 35419554
Mitochondrial Drp1 recognizes and induces excessive mPTP opening after hypoxia through BAX-PiC and LRRK2-HK2 [ Cell Death Dis, 2021, 12(11):1050]	PubMed: 34741026

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。