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Bafilomycin A1 (Synonyms: NSC 381866)

Catalog No.GC17597

La bafilomicina A1 (BafA1) es un inhibidor especÍfico y reversible de la H+-ATPasa vacuolar (V-ATPasa) con valores IC50 de 4-400 nmol/mg.

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Bafilomycin A1 Chemical Structure

Cas No.: 88899-55-2

Tamaño Precio Disponibilidad Cantidad
500µg
105,00 $
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1mg
200,00 $
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5mg
840,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 8 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1, 2]:

Cell lines

Eosinophils

Preparation Method

Circulating eosinophils were purified from donors with eosinophils >35 per μL of blood. Eosinophil preparations with purity >98% and viability ~98% were used.

Reaction Conditions

Eosinophils were cultured at 1 × 106/mL in complete medium (RPMI 1640 plus 10% fetal bovine serum) with IL3 (2 ng/mL) or IL5 (2 ng/mL) both cytokines from BD Biosciences for 20 h, and were then washed and cultured with complete medium (no IL3 or IL5) on coated heat-aggregated immunoglobulins-G (HA-IgG or IgG) or without IgG as previously described.

Applications

Bafilomycin-A1 could be used to show the impact of autophagolysosome formation on eosinophil cytolysis. Treated IL3- and IL5-primed eosinophils with bafilomycin-A1 before interaction with IgG, and then measured cytolysis using rhodamine-110 (R110). Treatment with bafilomycin-A1 increased IL3-primed and IL5-primed eosinophil lysis by 50% and 100%, respectively, suggesting that autophagolysosome formation protects from cytolysis for both IL3- and IL5-primed eosinophils.

Animal experiment [3]:

Animal models

Lck-mTOR + CLP mice, WT + CLP mice, Lck-TSC1 mice

Preparation Method

Crossed TSC1loxp/loxp and mTORloxp/loxp mice with Lck-Cre mice (Cre expression under the control of lymphocyte-specific protein tyrosine kinase, Lck) to obtain the F1 generation Lck-Cre:mTORloxp/− mice and Lck-Cre:TSC1loxp/− mice, respectively. We interbred F1 generation mice in each group and obtained F2 generation Lck-Cre: mTORloxp/loxp and Lck-Cre;TSC1loxp/loxp mice. Littermates lacking Lck-Cre served as controls. Then mice were anesthetized, and the abdomen was opened surgically and the cecum was ligated halfway between the distal pole and the base. The cecal stump was punctured once with a 22-gauge needle. Put back the cecum and closed the abdomen. Administered 1 mL saline subcutaneously to each animal for fluid resuscitation. Animals in the sham group underwent the same surgical procedure without ligation or puncture. Bafilomycin A1 was administered intraperitoneally 1 h after the CLP operation.

Dosage form

1 mg/kg

Applications

Bafilomycin A1 could specifically block fusion of autophagosomes and lysosomes and attenuate the protective effects of mTOR deletion against CD4 + T cell apoptosis. In Lck-mTOR + CLP mice treated with bafilomycin A1, the apoptosis rate of CD4 + T cells was higher compared with mice that did not receive bafilomycin A1 and lower compared with mice in WT + CLP + bafilomycin A1 group.

References:

[1]. Esnault S, et al. IL-3 up-regulates and activates human eosinophil CD32 and αMβ2 integrin causing degranulation. Clin Exp Allergy. 2017 Apr;47(4):488-498.

[2]. Esnault S, et al. Autophagy Protects against Eosinophil Cytolysis and Release of DNA. Cells. 2022 Jun 2;11(11):1821.

[3]. Wang H, et al. mTOR deletion ameliorates CD4 + T cell apoptosis during sepsis by improving autophagosome-lysosome fusion. Apoptosis. 2022 Jun;27(5-6):401-408.

Background

Bafilomicina A1, un antibiótico macrólido aislado de la especie Streptomyces, es un inhibidor de la vacuolar H ATPasa (V-ATPasa). La bafilomicina A1 se ha utilizado para estudiar la autofagia como inhibidor de la fusión entre los autofagosomas y los lisosomas, así como también como inhibidor de la degradación lisosomal. Se une a la subunidad c del sector V0 del complejo V-ATPasa e inhibe la translocación H, lo que provoca una acumulación de H en el citoplasma de las células tratadas. La bafilomicina A1 inhibe el crecimiento celular y conduce a apoptosis y diferenciación. Estos efectos anticancerígenos se consideran atribuibles a la acidosis intracelular causada por la inhibición de V-ATPasa.[2]

El estudio in vitro de Bafilomicina A1 indicó que esta sustancia inhibe preferentemente el crecimiento in vitro de células pediátricas de leucemia linfoblástica aguda de células B. Se utilizaron diversas líneas celulares de leucemia, incluyendo 697, Nalm-6, RS4;11, NB4, HL-60, K562 y BV173 que representan la LLA-B (697, Nalm-6, RS4;11), la leucemia mieloide aguda (NB4, HL-60) y la leucemia mieloide crónica (K562 , BV173) para investigar el efecto de Bafilomicina A1. Las células se cultivaron en presencia de concentraciones crecientes de Bafilomicina A1 (0 nM, 0.5 nM y 1 nM). La proliferación celular se midió utilizando un ensayo MTT. Los resultados mostraron que Bafilomicina A1 ha sido frecuentemente utilizada como inhibidor para bloquear la fusión entre autofagosomas-lisosomas o para inhibir la actividad lisosomal a altas dosis (0.1–1 mμ). Mientras que una baja concentración de Bafilomicina A1 (1 nM) podría inactivar eficazmente y específicamente la autofagia y activar apoptosis en múltiples objetivos en las células pediátricas LLA-B.[3]

El estudio in vivo demostró que la Bafilomicina A1 puede prolongar la supervivencia en ratones con leucemia linfoblástica aguda de células B avanzada tratados con Bafilomicina A1 en comparación con los ratones control. Los recuentos de glóbulos rojos, concentración de hemoglobina y plaquetas en el grupo modelo de LLA-B se redujeron significativamente, pero se normalizaron en el grupo tratado con Bafilomicina A1. Los ratones del grupo modelo de LLA-B presentaron hepatomegalia y esplenomegalia severa en comparación con el grupo control. Sin embargo, el tamaño y peso del hígado y bazo en el grupo tratado con Bafilomicina A1 se normalizó en comparación al modelo de enfermedad. Los resultados mostraron que la Bafilomicina A1 inhibe drásticamente la implantación celular pediátrica LLA-B mediante la eliminación selectiva de las células leucémicas in vivo.[3]

References:
[1]. Yamamoto A, et al. Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells. Cell Struct Funct. 1998;23(1):33–42.
[2] Bowman EJ, et al. The bafilomycin/concanamycin binding site in subunit c of the V-ATPases from Neurospora crassa and Saccharomyces cerevisiae. J Biol Chem. 2004;279(32):33131–33138.
[3]. 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.

Chemical Properties

Cas No. 88899-55-2 SDF
Sinónimos NSC 381866
Chemical Name (3Z,5E,7R,8S,9S,11E,13E,15S,16R)-16-[(2S,3R,4S)-4-[(2R,4R,5S,6R)-2,4-dihydroxy-5-methyl-6-propan-2-yloxan-2-yl]-3-hydroxypentan-2-yl]-8-hydroxy-3,15-dimethoxy-5,7,9,11-tetramethyl-1-oxacyclohexadeca-3,5,11,13-tetraen-2-one
Canonical SMILES CC1CC(=CC=CC(C(OC(=O)C(=CC(=CC(C1O)C)C)OC)C(C)C(C(C)C2(CC(C(C(O2)C(C)C)C)O)O)O)OC)C
Formula C35H58O9 M.Wt 622.84
Solubility 5 mg/ml in DMSO or in menthanol Storage Desiccate at -20°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.6055 mL 8.0277 mL 16.0555 mL
5 mM 0.3211 mL 1.6055 mL 3.2111 mL
10 mM 0.1606 mL 0.8028 mL 1.6055 mL
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