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Bafilomycin A1 (Baf-A1)

Name: Bafilomycin A1 (Baf-A1)
Brand: Selleck Chemicals
SKU: S1413
Rating: 5 (288 reviews)

Catalog No.S1413

For research use only.

Bafilomycin A1(Baf-A1) is a vacuolar H⁺-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.

Bafilomycin A1 (Baf-A1) Chemical Structure

CAS No. 88899-55-2

Selleck's Bafilomycin A1 (Baf-A1) has been cited by 288 publications

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Proton Pump Signaling Pathway Map

Biological Activity

Description

Bafilomycin A1(Baf-A1) is a vacuolar H⁺-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.

Targets

H+-ATPase ^[1]
(Cell-free assay)

0.44 nM

In vitro

Bafilomycin A1 is a toxic macrolide antibiotic derived from Streptomyces griseus. Bafilomycin A1 inhibits the short circuit current induced by the outer mantle epithelium (OME). The IC50 and maximum inhibition dose of Bafilomycin A1 are 0.17 μM and 0.5 μM, respectively. ^[2] In addition, Bilomycin A1 inhibits the acid influx with an IC50 value of 0.4 nM. Bafilomycin A1 inhibits the acidification dose-dependently resulting in a lower quenching, and thus a higher fluorescence. ^[3] Bafilomycin A1 prevents the vacuolization of Hela cells induced by H. pylori, with an inhibitory concentration giving 50% of maximal (ID50) of 4 nM. Bafilomycin A1 is also very efficient in restoring vacuolated cells to a normal appearance. ^[4] Bafilomycin A1 also affects the transport of endocytosed material from early to late endocytic compartments. Bafilomycin not only dissipates the low endosomal pH but also blocks transport from early to late endosomes in HeLa cells. ^[5] Bafilomycin A1 at doses of 0.1-1 μM completely inhibits the acidification of lysosomes revealed by the incubation with acridine orange in BNL CL.2 and A431 cells. ^[6] When Bafilomycin A1 is added to Hanks' balanced salt solution, endogenous protein degradation is strongly inhibited and numerous autophagosomes accumulated in H-4-II-E cells. Bafilomycin A1 also prevents the appearance of endocytosed HRP in autophagic vacuoles. ^[7]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

human H4 cells	MoXQSpVv[3Srb36gZZN{[Xl?	NHS1SnQxNjRizszN	NXXydpRHOjRiaB?=	NVn4TZI2UW6mdXP0bY9vKG:oIHzp[4h1KGOqYXnuJFMuT0[SIHzleoVtKGmwIHj1cYFvKEh2IHPlcIx{KGG2IECuOEB2VSCjZoTldkAzPCCqcoOgZpkhcGmpaDD0bJJwfWeqcIX0JIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3C7IILlcIF1cX[nIITvJINwdnS{b3y=	M2XpNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEK0OVg1Lz5zOECyOFU5PDxxYU6=
RAW 264.7 cells	M4HUVWZ2dmO2aX;uJIF{e2G7	M1q2bVExOCCwTR?=		M{DhdGFvfGmvaXPyc4Jq[WxiYXP0bZZqfHliYXfhbY5{fCCVYXztc45mdGyjIHXueIVzcWOjIGT5dIhqdXW{aYXtJFE1ODJ6IHnu[oVkfGWmIHnuJHJCXyB{NkSuO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[YQhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36gbY4hcW6oZXP0[YQh[2WubIOgZZQhOTByIH7N	M4DCbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7M{C3N\|U6Lz5zOUOwO\|M2QTxxYU6=
mouse RAW264.7 cells	M1PXSWFxd3C2b4Ppd{Bie3OjeR?=	Mn:4NVAxKG6P	MoP4NVYhcA>?	M{LvbGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XO\|ZYPz[YQh[XNibHH0[UBieG:ydH;0bYMh[2WubIOgZZQhOTByIH7NJIFnfGW{IEG2JIhzeyC3c3nu[{Bidm6neHnuJHYueHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{BjgSCobH;3JIN6fG:vZYTyfS=>	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTNyN{O1PUc,OTl\|MEezOVk9N2F-
human HeLa cells	MWXGeY5kfGmxbjDhd5NigQ>?	NV21bpdxPDByIH7N		NFfzdodKdmS3Y4Tpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIFjlUIEh[2WubIOg[ZhxemW\|c3nu[{BGT0[SLVzDN{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDMR\|MuOiCuZY\lcEBifCB2MECgcm0>	NHnJNGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5NVk1QSd-MUizPVE6PDl:L3G+
human MCF7 cells	MUjGeY5kfGmxbjDhd5NigQ>?		NFn5eVE1KGh?	NGn1OZVKdmirYnn0bY9vKG:oIILhdIFugWOrbj3pcoR2[2WmIHH1eI9xcGGpeTDpckBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochTUeIUD3MR\|Mh[XO\|ZYPz[YQh[XNiZHXjdoVie2ViaX6gSWdHWCCuZY\lcJMh[XRiMUCwJI5OKGGodHXyJFQhcHK\|IHL5JHdme3Sncn6gZoxwfHSrbnegdoVt[XSrdnWgeI8h[2:wdILvcC=>	NHe4Nno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MECyPFE{PCd-MkCwNlgyOzR:L3G+
RAW 264.7 cells	Mn7KRoFkfGW{aXPp[IFtKGGldHn2bZR6KGG\|c3H5	NFjySXgyODBibl2=	NUXqPYxFOTZiaB?=	MVzCZYN1\XKrY3nkZYwh[WO2aY\peJkh[WejaX7zeEBU[Wyvb37lcIxiKGWwdHXybYNiKFS7cHjpcZVzcXWvIEG0NFI5KGmwZnXjeIVlKGmwIGLBW{AzPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG\|ZTDpckBj[WO2ZYLpZYwh\3Kxd4ToJJlq\WymIHH0JFExOCCwTTDh[pRmeiBzNjDodpMheG:\|dHnu[oVkfGmxbjDifUBndG:5IHP5eI9u\XS{eTDpckBxemW\|ZX7j[UBw\iBzMDD1[{9udCCxZjDpcpRz[WOnbHz1cIFzKHKncHzpZ4F1cW:wIHnubIk>	NUnnOZVYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmzNFc{PTlpPkG5N\|A4OzV7PD;hQi=>
RAW 264.7 cells	MknuRY51cW2rY4LvZolidCCjY4Tpeol1gSCjc4PhfS=>	NG[3bG8yODBibl2=		NGTCeolCdnSrbXnjdo9jcWGuIHHjeIl3cXS7IHHnZYlve3RiU3HscY9v\WyuYTDlcpRmemmlYTDUfZBpcW23cnn1cUAyPDB{ODDpcoZm[3SnZDDpckBTSVdiMk[0Mlch[2WubIOgZZN{\XO\|ZXSgZZMhcW6lcnXhd4VlKG6rdILpZ{BwgGmmZTDwdo9lfWO2aX;uJIlvKGmwZnXjeIVlKGOnbHzzJIF1KDFyMDDuUS=>	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTNyN{O1PUc,OTl\|MEezOVk9N2F-
RAW 264.7 cells	NIrGWGZCdnSrbXnjdo9jcWGuIHHjeIl3cXS7IHHzd4F6	M3;pNlExOCCwTR?=	MW[zNEBucW6\|	NWjk[I9TSW62aX3pZ5Jw[mmjbDDhZ5Rqfmm2eTDh[4FqdnO2IGPhcI1wdmWubHGg[Y51\XKrY3GgWJlxcGmvdYLpeY0hOTRyMkigbY5n\WO2ZXSgbY4hWkGZIEK2OE44KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZoFkfGW{aXHsJJJmeGyrY3H0bY9vKGG2IEGwNEBvVSC2cnXheIVlKDNyIH3pcpMh[mWob4LlJIlv\mWldHnvckBu\WG\|dYLl[EBi\nSncjCyJJRwKDF4IHjyd{Bxd3O2aX7m[YN1cW:wIHL5JIZtd3diY4n0c41mfHK7	MlfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl\|MEezOVkoRjF7M{C3N\|U6RC:jPh?=
rat 3Y1 cells	MnnoSpVv[3Srb36gZZN{[Xl?			MmXJTY5lfWO2aX;uJI9nKG2xcoDoc4xw\2mlYXygZ4hidmenczDpckBz[XRiM2mxJINmdGy\|IHHzd4V{e2WmIHHzJIVtd26pYYTpc44hd2ZiY3XscJM>	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTdyMUm2N{c,Ojl5MEG5OlM9N2F-
human Huh7.5.1 cells	NVjjRVd[SW62aY\pdoFtKGGldHn2bZR6		NH;3ZVU{KGh?	M1PTNmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhEXiCpZX7veJlx\SB{YTDKSmguOSCrbjDoeY1idiCKdXi3MlUvOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[geolz[WxiZX70dpkhfXBidH:gN{BpenNiYomgcJVkcW[ncnHz[UBie3OjeR?=	Mof3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|OU[2PFMoRjJ4M{m2Olg{RC:jPh?=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	Ret / EGFR / p75 NGFR	21559479
Growth inhibition assay	Cell viability	20534000
Immunofluorescence	AIF ; LC3	25512644 24532803
ELISA	TNF-alpha	26240140

In vivo

Bafilomycin A1 (1 μM and 0.1 μM) completely inhibits the resorptive activity of cultured osteoclasts. ^[8] Bafilomycin A1 dose-dependently inhibits the rate of Na+ uptake in young tilapia with a Ki of 0.16 μM. ^[9]

Protocol (from reference)

Kinase Assay: ^[2]	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, 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 the specific V-ATPases inhibitor Bafilomycin A1.
Cell Research: ^[4]	Cell lines: HeLa cells Concentrations: ~20 nM Incubation Time: 20 hours Method: H. pylori bacteria extract is treated with inhibitors, before addition to HeLa cells, as follows: DCCD 10 mM for 1 hour at 30 ºC; NBD-CI 100 μM for 1 hour at 30 ºC and the reaction is blocked with glycine 10 mM final concentration; NEM 275 μM for 1 hour at 30 ºC and the reaction is blocked by addition of β-mercaptoethanol 275 mM; Mg-ATP 14 μM for 1 hour at 0 ºC; 100 μM KNO₃ and 14 μM Mg-ATP for 1 hour at 30 μM; NaCO₃ 100 μM, pH 11 for 1 hour at 0 ºC. The bacterial extract is then added to cell with a 40-fold dilution at a final concentration of 0.65 mg/mL. Controls are HeLa cells incubated with untreated bacterial extracts and cells treated with inhibitor Bafilomycin A1 under the same conditions as bacterial extracts, at the same concentrations or after a 40-fold dilution. The vacuotating activity of the bacterial extracts is assayed.
Animal Research: ^[9]	Animal Models: Young (approximately 9 days old) Mozambique tilapia, Oreochromis mossambicus Dosages: 10 μM Administration: --

References

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Solubility (25°C)

In vitro	DMSO	6 mg/mL (9.63 mM)
	Water	Insoluble
	Ethanol	Insoluble

Chemical Information

Molecular Weight	622.83
Formula	C₃₅H₅₈O₉
CAS No.	88899-55-2
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
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

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Frequently Asked Questions

Question 1:
How to dissolve it？

Answer:
S1413 Bafilomycin A1(Baf-A1) is soluble in DMSO at 6 mg/ml. Please do not use alcohols as solvent, because this compound will degrade in alcohols.

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