BAI1

製品コードS8865 バッチS886501

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
* <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 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.
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. BAI1 binds to monomeric BAX at a novel allosteric site. BAI1 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, BAI1 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. BAI1 selectively inhibits BAX-dependent cell death^[1].

製品説明

BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.

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. BAI1 binds to monomeric BAX at a novel allosteric site. BAI1 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, BAI1 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. BAI1 selectively inhibits BAX-dependent cell death^[1].

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

[1] Garner TP, et al. Nat Chem Biol. 2019, 15(4):322-330.

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：

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
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。

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