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Bafilomycin A1/巴佛洛霉素A1 {[allProObj[0].p_purity_real_show]}

貨號:A614767 同義名: BafA1; NSC 381866

Bafilomycin A1是一種空泡H+-ATP酶抑制劑,IC50為0.44 nM,同時可抑制自噬并誘導細胞凋亡。

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Bafilomycin A1/巴佛洛霉素A1 化學結構 CAS號:88899-55-2
Bafilomycin A1/巴佛洛霉素A1 化學結構
CAS號:88899-55-2
Bafilomycin A1/巴佛洛霉素A1 3D分子結構
CAS號:88899-55-2
Bafilomycin A1/巴佛洛霉素A1 化學結構 CAS號:88899-55-2
Bafilomycin A1/巴佛洛霉素A1 3D分子結構 CAS號:88899-55-2
規格 價格 會員價 庫存 數量
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Bafilomycin A1/巴佛洛霉素A1 純度/質量文件 產品僅供科研

貨號:A614767 標準純度: {[allProObj[0].p_purity_real_show]}
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產品名稱 ATPase 其他靶點 純度
(-)-Blebbistatin 99%+
PF 03716556 ++++

H+/K+-ATPase, pIC50: ~6.5

99%
Esomeprazole sodium ? 98%
BTB06584 ? 99%
Ciclopirox ? 97%
CB-5083 ++++

p97 AAA ATPase, IC50: 11 nM

99%+
Ciclopirox olamine ? 99%
Brefeldin A +++

ATPase (HCT 116), IC50: 0.2 μM

99%+
Oligomycin A ? 99%
Sodium orthovanadate +++

(Na,K)-ATPase, IC50: 40 nM

25-28%V
Golgicide A ? 99%+
1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多,抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用,但抑制強度暫時沒有相關數據。
產品名稱 Autophagy 其他靶點 純度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

95%
Hydroxychloroquine sulfate ? 99%
Valproic acid sodium ? HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 ? 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
Lys05 ? 99%+
1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多,抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用,但抑制強度暫時沒有相關數據。
產品名稱 Proton Pump 其他靶點 純度
Zinc pyrithione ? 98+%
PF 03716556 ++++

H+/K+-ATPase, pIC50: ~6.5

99%
Lansoprazole ? 98%
Esomeprazole Magnesium ? 98%+
Rabeprazole ? 99%+
Ilaprazole ? TOPK 97%
Bafilomycin A1 ++++

H+-ATPase, IC50: 0.44 nM

99%
Pantoprazole sodium ? 98%
(R)-Lansoprazole ? 98%
Tenatoprazole ? 99%+
Omeprazole ? 98%
1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多,抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用,但抑制強度暫時沒有相關數據。

Bafilomycin A1/巴佛洛霉素A1 生物活性

靶點
  • Proton Pump

    H+-ATPase, IC50:0.44 nM

描述 Bafilomycin A1, a macrolide antibiotic, is a potent and selective inhibitor of V-type H+-ATPase, and could disrupt pH regulation[1][2]. Bafilomycin A1 also showed moderate inhibition on ElE2 ATPases like K+-dependent (Kdp) ATPase from Escherichia coli, the Na+,K+-ATPase from ox brain, and the Ca2+-ATPase from sarcoplasmic reticulum, but F1Fo ATPases from bacteria and mitochondria are not affected by Bafilomycin A1[1]. Bafilomycin A1 can disrupt both autophagosome-lysosome fusion and autolysosome acidification constitute late steps in the autophagic process necessary to maintain functional autophagic flux and cellular homeostasis. Bafilomycin A1 induced a significant increase in cytosolic calcium concentration and disrupted Ca-P60A/SERCA-mediated fusion[3].
作用機制 Bafilomycin A1 disrupts autophagic flux by independently inhibiting V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion.[3]

Bafilomycin A1/巴佛洛霉素A1 細胞實驗

Cell Line
Concentration Treated Time Description References
Bovine brain V-ATPase 0.006 nM, 0.018 nM, 0.06 nM, 0.18 nM, 0.6 nM, 6 nM Bafilomycin A1 nearly completely inhibited the proton pumping activity of V-ATPase at nanomolar concentrations Nat Commun. 2021 Mar 19;12(1):1782.
HeLa cells 100 nM 5 h BafA 1 treatment increased the area of LAMP1-positive structures, indicating inhibition of lysosomal degradation capacity. Autophagy. 2018;14(8):1435-1455.
U2OS cells 100 nM 5 h BafA 1 treatment increased the area of LAMP1-positive structures, indicating inhibition of lysosomal degradation capacity. Autophagy. 2018;14(8):1435-1455.
Mouse bone marrow-derived macrophages 200 nM 2 h Induction of SQSTM1 accumulation in mouse bone marrow-derived macrophages by serum starvation and BafA treatment Autophagy. 2023 Oct;19(10):2789-2799.
EBV-transformed B cells 200 nM 2 h Induction of SQSTM1 accumulation in EBV-transformed B cells by serum starvation and BafA treatment Autophagy. 2023 Oct;19(10):2789-2799.
Jurkat cells 200 nM 2 h Induction of SQSTM1 accumulation in Jurkat cells by serum starvation and BafA treatment Autophagy. 2023 Oct;19(10):2789-2799.
U2OS cells 200 nM 2.5 h To investigate the effect of BafA1 on autophagosome-lysosome fusion, the results showed that BafA1 treatment for 2.5 h does not inhibit fusion between autophagosomes and lysosomes, but leads to the accumulation of LC3-positive material inside autolysosomes. Autophagy. 2022 Dec;18(12):3004-3022.
Primary rat cortical neurons 10 nM 24 h To assess the effects of Bafilomycin A1 on cellular bioenergetics, the results showed that Bafilomycin A1 significantly inhibited key parameters of mitochondrial function and increased mtDNA damage. Redox Biol. 2017 Apr;11:73-81.

Bafilomycin A1/巴佛洛霉素A1 動物研究

Dose Mice: 0.1 mg/kg, 1 mg/kg[4] (i.p.); 10 mg/kg[5] (intratumoral)
Administration i.p.

Bafilomycin A1/巴佛洛霉素A1 參考文獻

[1]Bowman EJ, Siebers A, 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 Nov;85(21):7972-6.

[2]van Schalkwyk DA, Chan XW, et al. Inhibition of Plasmodium falciparum pH regulation by small molecule indole derivatives results in rapid parasite death. Biochem Pharmacol. 2010 May 1;79(9):1291-9.

[3]Mauvezin C, Neufeld TP, 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):1437-8.

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

[5]Yan Y, Jiang K, et al. Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways. Sci Rep. 2016 Nov 15;6:37052.

Bafilomycin A1/巴佛洛霉素A1 實驗方案

計算器
存儲液制備 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.03mL

1.61mL

0.80mL

16.06mL

3.21mL

1.61mL

Bafilomycin A1/巴佛洛霉素A1 技術信息

CAS號88899-55-2
分子式C35H58O9
分子量 622.83
SMILES Code C[C@H]([C@](O[C@@H]1C(C)C)(C[C@@H](O)[C@@H]1C)O)[C@H](O)[C@@H]([C@](OC(/C(OC)=C/C(C)=C\[C@@H](C)[C@@H](O)[C@@H](C)C2)=O)([H])[C@H](/C=C/C=C2\C)OC)C
MDL No. MFCD06795130
別名 BafA1; NSC 381866
英文名稱(3Z,5Z,7R,8S,9S,11E,13E,15S,16R)-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
運輸藍冰
存儲條件

In solvent -20°C: 3-6個月 -80°C: 12個月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO 中的溶解度 : ≥ 100 mg/mL (160.56 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

請根據您的動物給藥指南選擇適當的溶解方案。
以下溶解方案都請先按照體外實驗的方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結果的可靠性,澄清的儲備液可以根據儲存條件,適當保存;體內實驗的工作液,建議現用現配,當天使用; 以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比;如在配制過程中出現沉淀、析出現象,可以通過加熱和/或超聲的方式助溶
方案 一
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