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Bafilomycin A1.

V-ATPase抑制剂,Bafilomycin A1，一种从链霉菌属物种中分离的大环内酯类抗生素，是特异的 vacuolar-type H+ ATPase 抑制剂。

目录号: PC16220 纯度: ≥98%

CAS No. :88899-55-2

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中文名称	Bafilomycin A1.
中文别名	巴佛洛霉素 A1;巴弗洛霉素A1;巴佛罗霉素A1;巴佛洛霉素 A1, 来源于灰色链霉菌;维生素D2;Bafilomycin A1 巴弗洛霉素A1;巴佛洛霉素A1 Solarbio
英文名称	Bafilomycin A1
英文别名	BAFILOMYCIN A1;BAFILOMYCIN A1, STREPTOMYCES GRISEUS;Bafilomycin A1 from Streptomycesgriseus, 10 ug;(3Z,5E,7R,8S,9S,11E,13E,15S,16R)-8-Hydroxy-16-((1S,2R,3S)-2-hydroxy-1-methyl-3-((2R,4R,5S,6R)-tetrahydro-2,4-dihydroxy-5;BafilomycinA1fromStreptomycesgriseus;21-O-de(3-carboxy-1-oxo-2-propenyl)-2-demethyl-2-methoxy-24-methyl-hygrolidin;Bafilomycin A1 (NSC 381866);(3Z,5E,7R,8S,9S,11E,13E,15S,16R)-8-Hydroxy-16-[(1S,2R,3S)-2-hydroxy-1-Methyl-3-[(2R,4R,5S,6R)-tetrahydro-2,4-dihydroxy-5-Methyl-6-(1-Methylethyl)-2H-pyran-2-yl]butyl]-3;bafilomycin;Bafilomycin A1 from Streptomyces griseus;Bafilomycin A
Cas No.	88899-55-2
分子式	C₃₅H₅₈O₉
分子量	622.83
包装储存	-80°C, protect from light

生物活性

Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H-ATPase (V-ATPase) with IC₅₀ values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.

性状

Solid

IC50 & Target[1][2]

Macrolide

体外研究(In Vitro)

Bafilomycin A1 is treated to different types of membrane ATPases with the I₅₀ of 400 nmol/mg, 4 nmol/mg and 50 nmol/mg for the vacuolar ATPases of a fungus (N. crassa), a plant (Z. mays), and an animal (bovine abrenal medulla). The I₅₀ values refer as μmol of Bafilomycin A1 per mg of protein giving 50% inhibition of ATPase activity.
Bafilomycin A1 ((-)-Bafilomycin A1) disrupts autophagic flux by inhibiting both V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion.
Bafilomycin A1 at a low concentration (1 nM) effectively and specifically inhibits and kills pediatric B-cell acute lymphoblastic leukemia cells. It targets both early and late stages of the autophagy pathway, mitochondria and induces caspase-independent apoptosis. Bafilomycin A1 induces the binding of Beclin 1 to Bcl-2, which further inhibits autophagy and promotes apoptotic cell death.
The growth of the BEL-7402 hepatocellular carcinoma and HO-8910 ovarian cancer cell lines are retarded and the metastatic potential is inhibited by Bafilomycin A1. Transmission electron microscopy and assays of capsase-3 and -9 suggest that Bafilomycin A1 induces apoptosis.
Bafilomycin A1 inhibits the growth of a variety of cultured cells dose-dependently, including golden hamster embryo and NIH-3T3 fibroblasts, whether or not they are transformed, and PC12 and HeLa cells. The IC₅₀ of Bafilomycin A1 for inhibition of cell growth ranges from 10 to 50 nM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Chronic treatment with low-dose Bafilomycin A1 (0.1 mg/kg) slightly inhibits the tumor volume, but the final tumor volume does not differ significantly from the control. However, chronic treatment with high dose Bafilomycin A1 (1 mg/kg) inhibits the tumor growth significantly, compared with controls, after 21 days.
Bafilomycin A1 (0.1 mg/kg or 1 mg/kg; i.p. daily for 3 days) extends the survival of B-cell acute lymphoblastic leukemia (B-ALL) xenograft mice with advanced disease.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-80°C, protect from light

结构分类

来源

Streptomyces griseus strains

参考文献

[1]. Bowman EJ, et al. Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells. Proc Natl Acad Sci U S A. 1988;85(21):7972-7976. [Information]

[2]. Mauvezin C, et al. Bafilomycin A1 disrupts autophagic flux by inhibiting both V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion. Autophagy. 2015;11(8):1437-1438. [Information]

[3]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015;100(3):345-356. [Information]

[4]. Yoshimori T, et al. Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, inhibits acidification and protein degradation in lysosomes of cultured cells. J Biol Chem. 1991;266(26):17707-17712 [Information]

[5]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015 Mar;100(3):345-56. [Information]

[6]. Lu X, et al. Bafilomycin A1 inhibits the growth and metastatic potential of the BEL-7402 liver cancer and HO-8910 ovarian cancer cell lines and induces alterations in their microRNA expression. Exp Ther Med. 2015 Nov;10(5):1829-1834. [Information]

[7]. Ohkuma S, et al. Inhibition of cell growth by bafilomycin A1, a selective inhibitor of vacuolar H(+)-ATPase. 体外研究 Cell Dev Biol Anim. 1993 Nov;29A(11):862-6. [Information]

[8]. Ohta T, et al. Bafilomycin A1 induces apoptosis in the human pancreatic cancer cell line Capan-1. J Pathol. 1998 Jul;185(3):324-30. [Information]

[9]. Cattani L, et al. Bafilomycin A1 and intracellular multiplication of Legionella pneumophila. Antimicrob Agents Chemother. 1997;41(1):212-214. [Information]

[10]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015 Mar;100(3):345-56. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (160.56 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6056 mL	8.0279 mL	16.0557 mL
5 mM	0.3211 mL	1.6056 mL	3.2111 mL
10 mM	0.1606 mL	0.8028 mL	1.6056 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months (protect from light)。-80°C 储存时，建议在 6 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.01 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.01 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.34 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.34 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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