Bafilomycin A1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bafilomycin A1 是一种从链霉菌属物种中分离出来的大环内酯类抗生素，也是液泡 V-ATP 酶的抑制剂。

Bafilomycin A1 is a macrolide antibiotic isolated from the Streptomyces species and an inhibitor of vacuolar V-ATPase.

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.

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.

NSC 381866

Membrane Transporter/Ion Channel

Proton Pump

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Metabolic Disease

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88899-55-2

622.83

C??H??O?

>98% (HPLC)

N/A

O[C@H]([C@H](C)/C=C(C)/C=C1OC)[C@@H](C)C/C(C)=C/C=C\[C@H](OC)C([C@@H](C)[C@H]([C@@H]([C@@]2(O)C[C@@H](O)[C@H](C)[C@@H]([C@H](C)C)O2)C)O)OC/1=O

(3E,5E,7R,8S,9S,11E,13Z,15S)-16-((2S,3R,4S)-4-((2R,4R,5S,6R)-2,4-dihydroxy-6-isopropyl-5-methyltetrahydro-2H-pyran-2-yl)-3-hydroxypentan-2-yl)-8-hydroxy-3,15-dimethoxy-5,7,9,11-tetramethyloxacyclohexadeca-3,5,11,13-tetraen-2-one

(-20℃)

With Ice Pack

≥ 2 years