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Brefeldin A (BFA chemical) Inhibidor del transporte de proteínas

Name: Brefeldin A (BFA chemical)
Brand: Selleck Chemicals
SKU: S7046
Rating: 5 (90 reviews)

Cat. No.S7046

Brefeldin A (BFA) es un antibiótico de lactona e inhibidor de ATPasa para el transporte de proteínas con una IC50 de 0,2 The HTML tag in the content has been properly ignored, and it has been translated directly, not converted: en células HCT 116, induce la diferenciación de células cancerosas y la apoptosis. También podría mejorar la eficiencia de la HDR (reparación dirigida por homología) y ser un potenciador de la HDR mediada por CRISPR. Brefeldin A también es un inhibidor de la autofagia y la mitofagia.

Brefeldin A (BFA chemical) ATPase inhibidor Chemical Structure

Estructura química

Peso molecular: 280.36

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Control de calidad

Lote: Pureza: 99.94%

99.94

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Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	PMID
PC12	Function Assay	2 μM	1 h		inhibits the L-DOPA (20 μM)-induced transient ERK1/2 phosphorylation	26363191
C2C12	Function Assay	1 μg/ml	1 h		abolishes cytokine release from C2C12 myotubes	26291279
MEFs WT	Function Assay	5 μM	20 min		causes resident enzymes such as NAGT-GFP, to diffuse back to the ER	26196023
MEFs VAMP7 KO	Function Assay	5 μM	20 min		causes resident enzymes such as NAGT-GFP, to diffuse back to the ER	26196023
SMCs	Function Assay	10 µg/ml	0-12 h	DMSO	shows a trend towards a higher concentration of the ER/SR network in the perinuclear area	26172080
SMCs	Function Assay	10 µg/ml	0-12 h	DMSO	causes a transient Ca2+ release from the ER/SR	26172080
HEMC-1	Function Assay	0.1 µg/ml	24 h		causes a higher inhibitory effect on exocytosis than nocodazole	25972759
HUVEC	Function Assay	10 μM	1 h	DMSO	abolishes hypoxia-induced release of ATP from apical and basolateral surfaces	25956988
HUVEC	Function Assay	10 μM	1 h	DMSO	increases the number and intensity of fluorescent areas especially in perinuclear space	25956988
Caco-2	Function Assay	2.5 μM	30 min		attenuates the TGF-β1-mediated increase in SERT function	25954931
NRK	Function Assay	200 ng/ml	4 h	DMSO	rescues mitotic progression	25948586
HeLa	Function Assay	200 ng/ml	3 h	DMSO	induces the artificial break-up of the Golgi complex	25948586
COS	Function Assay	1 μg/ml	3 h		completely disperses the AP-1 signal	25915900
DF1	Function Assay	1 μM	48 h	DMSO	disperses the exogenous CSGalNAcT2 protein	25807054
nHDFs	Function Assay	1 μM	2 h		prevents the assembly of cytosolic coat proteins onto Golgi membranes	25772616
FRT	Function Assay	5 μg/ml	2 h		blocks trafficking through the Golgi complex by inhibiting ER-to-Golgi transport	25767115
FRT	Function Assay	5 μg/ml	2 h		prevents the increase in cleaved α subunits when [Na+]i was reduced	25767115
HepG2	Function Assay	1 µM	24 h	DMSO	decreases the level of PXR mRNA	25616597
SMCs	Function Assay	1μg/mL	3 h		accumulates CNPY2 protein in the ER compartment and no longer co-localized with the Golgi marker	25589425
OB-6	Apoptosis Assay	2.7 μM	48 h		induces apoptosis	25532480
iPSC-CMs	Function Assay	500 ng/ml	48 h		increases the intensity of the higher mobility LAMPs at the cost of the lower mobility species	25488666
SP-Nluc	Function Assay	5 mg/mL	6 h	DMSO	causes an increase in reporter activity in the parasite	25392998
PEXEL-Nluc	Function Assay	5 mg/mL	6 h	DMSO	causes an increase in reporter activity in the parasite	25392998
H1299	Function Assay	10 μg/ml	24 h		induces autophagy	25388970
MDA-MB-231	Cell Viability Assay	0–50 μg/mL	48 h		EC50 = 0.016 µg/mL	25356567
MDA-MB-231	Apoptosis Assay	0.1 μg/mL	4 h		induces apoptosis	25356567
MDA-MB-231	Growth Inhibition Assay	0.01/0.05 μg/mL	24 h		increases the fraction of sub-G1 cell debris	25356567
MDA-MB-231	Apoptosis Assay	0.05–1 μg/mL	24 h		induces PARP (poly ADP-ribose polymerase-1) cleavage	25356567
MDA-MB-231	Function Assay	0–50 μg/mL	24 h		inhibits the formation of 3D and 2D colonies	25356567
A172	Function Assay	10 μg/ml	4 h	DMSO	results in the retrograde transport of fluorescent granules	25239507
KMS-6	Function Assay	1 μM	24 h		exhibits half the secretion of galanin-LI as did the control	25229126
MEC	Function Assay	1 μM	1.5 h		causes a dramatic decrease in the surface VEGFR2	25228815
HEK293/hERG	Function Assay	10 μM	1 h		results in a time-dependent reduction mature hERG protein	25218469
RBE4	Apoptosis Assay	2 μM	3–24 h		induces apoptosis time dependently	25128025
RBE4	Function Assay	2 μM	3–24 h		increases the XBP1 protein levels after 3 and 6 h of treatment	25128025
RBE4	Function Assay	2 μM	3–24 h		increases active caspase-12 in a time-dependent manner	25128025
RBE4	Function Assay	2 μM	3–24 h		increases the levels of ROS time-dependently	25128025
RBE4	Function Assay	2 μM	3–24 h		induces a delayed depletion of the ER Ca2+ content at 6 h of incubation significantly	25128025
RBE4	Function Assay	2 μM	3–24 h		induces an overload of Ca2+ in the mitochondria in the first 6 h of incubation (p < 0.001) but Ca2+ levels in this organelle decreased after 12 h of incubation	25128025
Huh-7	Function Assay	1μg/mL	3–24 h		increases the level of APE1 in a time-dependent manner	25026174
HepG2	Function Assay	1μg/mL	3–24 h		increases the level of APE1 in a time-dependent manner	25026174
H838-LKB1	Function Assay	30 ng/ml	12/18 h		increases the protein levels of BiP	25011082
H838-KDLKB1	Function Assay	30 ng/ml	12/18 h		increases the protein levels of BiP	25011082
H838-KDLKB1	Function Assay	30 ng/ml	12/18 h		increases the levels of phosphorylated eIF2α (phospho-eIF2α)	25011082
3T3-L1	Function Assay	5 μg/ml	30 min		mimics the effects of insulin and causes robust phosphorylation of Akt (Ser 473) and phosphorylation of AS160 (Thr 642 and Ser 588)	24843827
3T3-L1	Function Assay	5 μg/ml	30 min		recapitulates insulin action with respect to regulating Akt activity and AS160 phosphorylation	24843827
3T3-L1	Function Assay	5 μg/ml	30 min		causes reversible redistribution of GLUT4	24843827
3T3-L1	Function Assay	5 μg/ml	1 h		causes redistribution of GLUT4 but not increase in glucose uptake	24843827
3T3-L1	Function Assay	5 μg/ml	1 h		causes phosphorylation of the FoxO1 transcription factor	24843827
HeLa	Function Assay	5 μg/ml	3 h		causes nuclear exclusion of the FoxO1 transcription factor and decreases transcription of FoxO1-regulated genes	24843827
HEK293	Function Assay	5 μg/ml	12 h		abolishes CMA-induced CRELD2 secretion	24687431
COS-1	Function Assay	5 µg/ml	24 h		restricts localization of NB in the perinuclear region	24671751
PRP	Function Assay	10 μM			abrogates SDF-1α-mediated CXCR7 externalization	24668750
RAW264.7	Apoptosis Assay	4 μM	48 h		attenuates the inhibition of ox-LDL-induced apoptosis and the facilitation of cholesterol efflux by Ac-hE-18A-NH2	24639032
MDMs	Apoptosis Assay	10 μg/ml	12/15 h		induces apoptosis	24556695
PMHs	Function Assay	10–20 μg/ml	24 h	DMSO	induced ER stress	24407242
PMHs	Apoptosis Assay	10–20 μg/ml	24 h	DMSO	increases cell death	24407242
HEK293/tau	Function Assay	5 μM	1/2/4 h		induces Golgi fragmentation	24368089
HEK293/tau	Function Assay	5 μM	3 h		induces tau hyperphosphorylation	24368089
ADF	Function Assay	10 μM	16 h		inhibits the ZnCl2-induced translocation of CRT	24228232
U373	Function Assay	10 μM	16 h		inhibits the ZnCl2-induced translocation of CRT	24228232
RKO-HIPK2i	Function Assay	10 μM	16 h		inhibits the ZnCl2-induced translocation of CRT	24228232
ADF	Function Assay	10 μM	6 h		impairs the DC activation	24228232
Huh7	Function Assay	5 μg/ml	4 h		abolishes the secretion of intracellular ApoB	24100140
Huh7	Function Assay	5 μg/ml	1 h		causes a significant increase in ApoB-crescents	24100140
Huh7	Function Assay	5–10 ng/ml	12 h		increases ApoB-crescents without inhibiting secretion	24100140
BAECs	Function Assay	5 μg/ml	0-4 h		induces the rapid dephosphorylation of eNOS at Ser1179	24085225
Macrophages	Function Assay	71 µM	6 h		inhibits lunasin internalization	24039740
Colo 205	Growth Inhibition Assay	0-5 μg/mL	48 h		inhibits cell growth in suspension cultures with an estimated IC50 of ~15 ng/mL	23973996
Colo 205	Function Assay	0.012-0.025 μg/mL	14 d		reduces the clonogenicity of Colo 205 CSCs	23973996
Colo 205	Apoptosis Assay	0.1 μg/mL	0-24 h		induces apoptosis of Colo 205 cells in suspension cultures	23973996
Colo 205	Function Assay	0.015 μg/mL	24 h		induces the expression of ER stress-related genes	23973996
Colo 205	Function Assay	0.015 μg/mL	24 h		inhibits the activity of MMPs	23973996
IBRS2	Function Assay	5 μg/ml	0.5 h	DMSO	disrupts the ERGIC and Golgi	23963534
IBRS2	Function Assay	5 μg/ml	0.5 h	DMSO	enhances FMDV infection	23963534
HeLa	Function Assay	2 μM	2 h		attenuates the TNF-induced secretion of IL-15	23950892
HFS	Function Assay	0-1 μg/ml	24 h		GLTP expression reaches a plateau at concentrations as low as 0.01 µg/ml	23894633
HFS	Function Assay	0.01 µg/ml	24 h		increases the expression of glycosphingolipid synthase genes at 6 h	23894633
OVCAR-3	Growth Inhibition Assay	1–15 μM	24 h		induces a loss of cell viability dose dependently	23826964
OVCAR-3	Function Assay	1–15 μM	24 h		induces nuclear damage	23826964
OVCAR-3	Apoptosis Assay	1-10 μM	4 h		induces the activation of apoptosis-related proteins	23826964
OVCAR-3	Apoptosis Assay	10 μM	24 h		induces activation of caspases	23826964
OVCAR-3	Function Assay	1–10 μM	24 h		induces disruption of the mitochondrial transmembrane potential	23826964
OVCAR-3	Function Assay	1–10 μM	24 h		induces formation of reactive oxygen species	23826964
OVCAR-3	Function Assay	1–10 μM	24 h		inhibits cell adhesion and migration	23826964
MKN45	Growth Inhibition Assay				IC50<0.001 μg/ml	23793342
LOVO	Growth Inhibition Assay				IC50=0.12 μg/ml	23793342
A549	Growth Inhibition Assay				IC50=0.04 μg/ml	23793342
MDA-MB-435	Growth Inhibition Assay				IC50<0.001 μg/ml	23793342
HepG2	Growth Inhibition Assay				IC50<0.001 μg/ml	23793342
HL-60	Growth Inhibition Assay				IC50<0.001 μg/ml	23793342
neural precursor cells	Function assay				Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay	17417631
HeLa	Function assay	100 uM	2 hrs		Dispersion of cis golgi marker betaCoP in human HeLa cells at 100 uM for 2 hrs	17563369
HeLa	Function assay	100 uM	2 hrs		Dispersion of cis golgi marker KDEL in human HeLa cells at 100 uM for 2 hrs	17563369
Vero	Function assay	10 ug/ml	5 mins		Inhibition of Arf1 in african green monkey Vero cells assessed as rapid AP-1 dispersal from golgi membranes at 10 ug/ml after 5 mins by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	5 mins		Inhibition of Arf1 in african green monkey Vero cells assessed as rapid GGA3 dispersal from trans golgi network at 10 ug/ml after 5 mins by immunofluorescence method	19182783
Vero	Function assay	10 uM	1 hr		Inhibition of GBF1 QNV deleted mutant in african green monkey Vero cells assessed as effect on change in golgi morphology at 10 uM after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 uM	1 hr		Inhibition of GBF1 QNV to AAA mutant in african green monkey Vero cells assessed as effect on change in golgi morphology at 10 uM after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	1 hr		Inhibition of Arf1 in african green monkey Vero cells assessed as decrease in Arf1-GTP levels at 10 ug/ml after 1 hr	19182783
Vero	Function assay	10 uM			Inhibition of GBF1 in african green monkey Vero cells assessed as inhibition of StxB-SS retrogade transport from endosomes to TGN at 10 uM by immunofluorescence method	19182783
Vero	Function assay	10 uM	1 hr		Inhibition of GBF1 in african green monkey Vero cells assessed as punctate and diffuse distribution of medial-Golgi marker giantin from TGN at 10 uM after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	1 hr		Inhibition of Arf1 in african green monkey Vero cells assessed as punctate and diffuse distribution of medial-Golgi marker giantin at 10 ug/ml after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	5 mins		Inhibition of Arf1 in african green monkey Vero cells assessed as rapid COPI redistribution from golgi at 10 ug/ml after 5 mins by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	1 hr		Inhibition of Arf1 in african green monkey Vero cells assessed as tubule formation from trans golgi network and endosomes before its dispersal at 10 ug/ml after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	1 hr		Inhibition of Arf1 in african green monkey Vero cells assessed as giantin positive punctate structures in contact with Sec31-positive ER exit site at 10 ug/ml after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml			Inhibition of Arf1 in african green monkey Vero cells assessed as inhibition of StxB-SS retrogade transport from endosomes to TGN at 10 ug/ml by immunofluorescence method	19182783
Vero	Function assay	10 uM	1 hr		Induction of GBF1 in african green monkey Vero cells assessed as punctate and diffuse distribution of cis-Golgi marker GM130 from TGN at 10 uM after 1 hr by immunofluorescence method	19182783
Vero	Function assay	10 ug/ml	1 hr		Inhibition of Arf1 in african green monkey Vero cells assessed as punctate and diffuse distribution of cis-Golgi marker GM130 at 10 ug/ml after 1 hr by immunofluorescence method	19182783
NRK	Function assay	7 uM	60 mins		Golgi-disturbing activity in golgi apparatus of rat NRK cells assessed as fusion of golgi membrane fusion with endoplasmic reticulum at 7 uM after 60 mins by Hoechst 3342 staining-based immunofluorescence microscopy	20189813
NCI60	Cytostatic assay				Cytostatic activity against human NCI60 cells by SRB assay, GI50=0.0206μM.	23805957
NCI60	Cytostatic assay				Cytostatic activity against human NCI60 cells by SRB assay, TGI=3.48μM.	23805957
HeLa R19	Antiviral assay	0.5 uM	7 hrs		Antiviral activity against Coxsackievirus B3 infected in human HeLa R19 cells assessed as inhibition of viral replication at 0.5 uM after 7 hrs by luciferase reporter gene assay	23805957
HeLa	Function assay	5 uM	30 to 60 mins		Induction of golgi apparatus disassembly in human HeLa cells at 5 uM after 30 to 60 mins by confocal microscopic analysis	23805957
Arabidopsis thaliana root cells	Function assay	90 uM	30 mins		Induction of morphological changes of golgi apparatus in Arabidopsis thaliana root cells expressing ST-YFP/VHAa1-RFP at 90 uM after 30 mins by confocal laser scanning microscopic analysis	23805957
HeLa R19	Antiviral assay	5 to 50 uM	7 hrs		Antiviral activity against Coxsackievirus B3 infected in human HeLa R19 cells assessed as inhibition of viral replication at 5 to 50 uM after 7 hrs by luciferase reporter gene assay	23805957
PC3	Function assay	50 nM	72 hrs		Potentiation of 3 nM docetaxel-induced cytotoxicity against human PC3 cells assessed as decrease in cell viability at 50 nM after 72 hrs by trypan blue exclusion assay	28462831
L02	Cytotoxicity assay		72 hrs		Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50<0.0004μM.	28494251
PC3	Antiproliferative assay		72 hrs		Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=0.068μM.	28494251
HT-29	Antiproliferative assay		72 hrs		Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.16μM.	28494251
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50=0.35μM.	28494251
LO2	Antiproliferative assay		72 hrs		Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay, IC50<0.001μM.	29524728
Bel7402	Antiproliferative assay		72 hrs		Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50=0.024μM.	29524728
HL60	Antiproliferative assay		72 hrs		Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.025μM.	29524728
PC3	Antiproliferative assay		72 hrs		Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=0.068μM.	29524728
Bel7402/5-FU	Antiproliferative assay		72 hrs		Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay, IC50=0.82μM.	29524728
HeLa	Function assay	18 uM	3 hrs		Inhibition of alkaline phosphatase secretion in human HeLa cells at 18 uM incubated for 3 hrs	31421965
VERO-E6	Function assay		48 hrs		Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging, IC50=0.02μM.	ChEMBL
VERO-E6	Function assay		48 hrs		Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=0.06μM.	ChEMBL
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Información química, almacenamiento y estabilidad

Peso molecular	280.36	Fórmula	C₁₆H₂₄O₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	20350-15-6	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Cyanein, Decumbin			Smiles	CC1CCCC=CC2CC(CC2C(C=CC(=O)O1)O)O

Solubilidad

In vitro
Lote:

DMSO : 56 mg/mL (199.74 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 125 mg/mL (445.85 mM) Calentado con baño de agua a 50°C; Ultrasonido;
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC₅₀/Ki	ATPase (HCT 116) 0.2 μM
In vitro	La Brefeldina A (BFA) es un metabolito fúngico que bloquea el transporte anterógrado entre el retículo endoplasmático y el aparato de Golgi, lo que provoca una distribución alterada de las proteínas de membrana. Cuando las células de cáncer de colon humano HCT 116 se tratan con este compuesto, se observan cambios morfológicos que indican diferenciación celular. Ejerce sus efectos citotóxicos principalmente induciendo la diferenciación y la apoptosis en las células tumorales. El tratamiento de las tiras con 20 μg/mL de BFA durante 6 horas anula completamente la relajación inducida por bradicinina en presencia de 10mM de indometacina y 30 μM de L-NOARG. El tratamiento con 20 μg/mL de este compuesto anula sustancialmente las disminuciones de [Ca²⁺]_i y tensión inducidas por bradicinina en el rango de concentraciones entre 1 nM y 1 mM. No tiene efecto sobre la elevación de [Ca²⁺]_i en células endoteliales inducida por bradicinina o sustancia P. La adición del metabolito fúngico no afecta la unión espontánea de GTPS dependiente de fosfolípidos a myr-rARF1, pero anula totalmente el intercambio catalizado por el extracto isotónico de retina (RIE), con una inhibición semimáxima a 2 μM. Previene una amplia variedad de vías de tráfico de membrana e inhibe una actividad de intercambio de nucleótidos de guanina específica del factor de ADP-ribosilación presente en las membranas de Golgi o en el citosol cerebral. La prevención completa por este compuesto sugiere fuertemente que el extracto de retina contiene un factor de intercambio de nucleótidos de guanina específico de ARF. La liberación de GTPS catalizada por el extracto isotónico de retina (RIE) de ambos factores de ADP-ribosilación (ARF) solo es parcialmente inhibida por BFA, incluso a 300 μM. Induce la fusión del aparato de Golgi con el RE y anula el efecto inhibidor del inhibidor de CERT HPA-12. El tratamiento con este compuesto, que induce la fusión del aparato de Golgi y el RE, rescata la prevención de la biosíntesis de esfingomielina inducida por limonoides. Su tratamiento de células CHO provoca un aumento de 2 a 3 veces en la síntesis de esfingomielina. Además de las células B-CLL, la BFA, según se informa, causa apoptosis en mieloma múltiple (U266, NCI-H929), Jurkat, HeLa, leucemia (HL60, K562, BJAB), colon (HT-29) y próstata, así como células de sarcoma quístico adenoide. La administración de 25 ng/mL de este compuesto bloquea completamente el crecimiento de las células HF4.9 y HF28RA, mientras que se requieren dosis más altas (75 ng/mL) para lograr el mismo efecto en las células HF1A3. La proliferación celular se inhibe en 24 horas de manera dosis-dependiente y, dependiendo de la línea celular, se observa una cesación casi completa de la incorporación de ³H-timidina a 50-75 ng/mL (26%, 76%, 87% de inhibición a 50 ng/ml y 75%, 87%, 92% de inhibición a 75 ng/mL para las células HF1A3, HF4.9 y HF28RA respectivamente. La muerte celular inducida por BFA es de manera dosis-dependiente utilizando el ensayo YO-PRO 1/PI. Podría mejorar la eficiencia de la HDR (reparación dirigida por homología) y es un potenciador de la HDR mediada por CRISPR.
In vivo	Brefeldina A (BFA), un antibiótico de lactona e inhibidor específico del tráfico de proteínas, bloquea el transporte de proteínas secretadas y de membrana desde el retículo endoplasmático al aparato de Golgi.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/10722169/ [2] https://pubmed.ncbi.nlm.nih.gov/11522609/ [3] https://pubmed.ncbi.nlm.nih.gov/8576155/ [4] https://pubmed.ncbi.nlm.nih.gov/22566693/ [5] https://pubmed.ncbi.nlm.nih.gov/17428536/ [6] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4461869/ [7] https://pubmed.ncbi.nlm.nih.gov/30110907/

Aplicaciones

Métodos	Biomarcadores	PMID
Western blot	p53 / GRP78	22859938
Immunofluorescence	MTP / GBF1 ErbB3 / Calnexin FMNL1 / GM130	26267806
Growth inhibition assay	Cell viability	28462831

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