Home Transmembrane Transporters Proton Pump inhibitor Bafilomycin A1 (Baf-A1)

연구용

Bafilomycin A1 (Baf-A1) V-ATPase inhibitor

제품 번호S1413

Bafilomycin A1 (Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM, and it is found to inhibit autophagy while inducing apoptosis.
Bafilomycin A1 (Baf-A1) Proton Pump inhibitor Chemical Structure

화학 구조

분자량: 622.83

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품질 관리 (Quality Control)

배치: 순도: >97%
97

함께 자주 사용되는 제품 Bafilomycin A1 (Baf-A1)

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세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
human H4 cells Function assay 0.4 μM 24 h Induction of light chain 3-GFP level in human H4 cells at 0.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control 18024584
RAW 264.7 cells Function assay 100 nM Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as increased nitric oxide production in infected cells at 100 nM 19307359
mouse RAW264.7 cells Apoptosis assay 100 nM 16 h Induction of apoptosis in mouse RAW264.7 cells assessed as late apoptotic cells at 100 nM after 16 hrs using annexin V-propidium iodide staining by flow cytometry 19307359
human HeLa cells Function assay 400 nM Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 400 nM 18391949
human MCF7 cells Function assay 4 h Inhibition of rapamycin-induced autophagy in human MCF7 cells expressing EGFP-LC3 assessed as decrease in EGFP levels at 100 nM after 4 hrs by Western blotting relative to control 20028134
RAW 264.7 cells Bactericidal activity assay 100 nM 16 h Bactericidal activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in bacterial growth yield at 100 nM after 16 hrs postinfection by flow cytometry in presence of 10 ug/ml of intracellular replication inhi 19307359
RAW 264.7 cells Antimicrobial activity assay 100 nM Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as increased nitric oxide production in infected cells at 100 nM 19307359
RAW 264.7 cells Antimicrobial activity assay 100 nM 30 mins Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as inhibition of bacterial replication at 100 nM treated 30 mins before infection measured after 2 to 16 hrs postinfection by flow cytometry 19307359
rat 3Y1 cells Function assay Induction of morphological changes in rat 3Y1 cells assessed as elongation of cells 29701963
human Huh7.5.1 cells Antiviral activity 3 h Antiviral activity against HCV genotype 2a JFH-1 in human Huh7.5.1 cells assessed as reduction of viral entry up to 3 hrs by luciferase assay 26396683
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 622.83 화학식

C35H58O9

 보관 (수령일로부터)
CAS 번호 88899-55-2 SDF 다운로드 원액 보관

동의어 N/A 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

용해도 (Solubility)

In vitro
배치:

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
H+-ATPase
(Cell-free assay)
0.44 nM
시험관 내(In vitro)
Bafilomycin A1 (Baf-A1) is a toxic macrolide antibiotic derived from Streptomyces griseus, which inhibits the short circuit current induced by the outer mantle epithelium (OME). The IC50 and maximum inhibition dose of this compound are 0.17 μM and 0.5 μM, respectively. In addition, it inhibits the acid influx with an IC50 value of 0.4 nM. It also inhibits the acidification dose-dependently resulting in a lower quenching, and thus a higher fluorescence. This compound prevents the vacuolization of Hela cells induced by H. pylori, with an inhibitory concentration giving 50% of maximal (ID50) of 4 nM, and is very efficient in restoring vacuolated cells to a normal appearance. It also affects the transport of endocytosed material from early to late endocytic compartments, not only dissipating the low endosomal pH but also blocking transport from early to late endosomes in HeLa cells. At doses of 0.1-1 μM, it completely inhibits the acidification of lysosomes revealed by the incubation with acridine orange in BNL CL.2 and A431 cells. When added to Hanks' balanced salt solution, endogenous protein degradation is strongly inhibited and numerous autophagosomes accumulated in H-4-II-E cells. It also prevents the appearance of endocytosed HRP in autophagic vacuoles.
키나아제 분석
ATPase enzyme activity assays
The ATPase enzyme assay medium contains 6 mM MgSO4, 50 mM HEPES (pH 7.4), 200 mM Na2SO3 (V-ATPase activator), 0.5 mM sodium ortho-vanadate (P-ATPase inhibitor), 0.5 mM sodium azide (F-ATPase inhibitor) and 3 mM Na2ATP. This medium (1.0 mL), with or without the addition of the V-type ATPase inhibitor bafilomycin A1 (Baf-A1), is incubated with the filtered homogenate (0.1 mL) for 60 minutes at 23–25 °C. The reaction is stopped by the addition of 1 mL of TCA 3%. Spectrometric blanks are prepared as for the enzyme assay with the exception that the tissue sample is added after the acid. Phosphate analysis is accomplished by adding 2 mL of 1-butanol and 0.2 mL molybdate solution (5 g ammonium molybdate, 22 mL H2SO4 to 100 mL). After vortexing for 15 seconds the solution is neutralised with 0.5 mL citrate solution (100 g/500 mL, pH 7.0) and again vortexed for 15 seconds. The solution is then centrifuged (2000 × g; 3 minutes) to separate the butanol phase and the absorbance of this phase is read at 400 nm. Standards of orthophosphate are prepared (0.1 μM–2.0 μM) and treated in the same way as the enzyme activity assays. Enzyme activity is expressed in μmol of orthophosphate liberated per hour and per milligram of protein. V-ATPase activity is considered to be the difference between the total ATPase activity measured in the presence of Na2SO3, sodium orthovanadate and sodium azide and the ATPase activity measured in the presence of these reagents and of this compound.
생체 내(In vivo)
Bafilomycin A1 (Baf-A1) (1 μM and 0.1 μM) completely inhibits the resorptive activity of cultured osteoclasts. This compound dose-dependently inhibits the rate of Na+ uptake in young tilapia with a Ki of 0.16 μM.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/8446034/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9811698/
  • [6] https://pubmed.ncbi.nlm.nih.gov/1832676/
  • [7] https://pubmed.ncbi.nlm.nih.gov/9639028/
  • [8] https://pubmed.ncbi.nlm.nih.gov/7817803/
  • [9] https://pubmed.ncbi.nlm.nih.gov/10574743/
  • [10] https://pubmed.ncbi.nlm.nih.gov/14713959/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot Ret / EGFR / p75 NGFR
S1413-WB1
21559479
Growth inhibition assay Cell viability
S1413-viability1
20534000
Immunofluorescence AIF LC3
S1413-IF1
25512644
ELISA TNF-alpha
S1413-ELISA1
26240140

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
How to dissolve it？

답변:
S1413 is soluble in DMSO at 6 mg/ml. Please do not use alcohols as solvent, because this compound will degrade in alcohols.