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Brefeldin A (BFA chemical) Protein Transport Inhibitor

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

Cat.No.S7046

Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.

Chemical Structure

Molecular Weight: 280.36

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel GluR
Other ATPase Inhibitors	(-)-Blebbistatin Thapsigargin CB-5083 Bufalin Sodium orthovanadate Golgicide A Saikosaponin D CDN1163 Ginsenoside Rb1 Periplocin

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 125 mg/mL (445.85 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.

In vivo Formulation Calculator (Clear solution)

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Chemical Information, Storage & Stability

Molecular Weight	280.36	Formula	C₁₆H₂₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	20350-15-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Cyanein, Decumbin			Smiles	CC1CCCC=CC2CC(CC2C(C=CC(=O)O1)O)O

Mechanism of Action

Targets/IC₅₀/Ki	ATPase (HCT 116) 0.2 μM
In vitro	Brefeldin A (BFA) is a fungal metabolite that blocks the forward transport between the endoplasmic reticulum and Golgi apparatus, causing an impaired distribution of the membrane proteins. When HCT 116 human colon cancer cell is treated with this compound, morphological changes indicating cell differentiation are observed. It exerts its cytotoxic effects mainly by inducing differentiation and apoptosis in tumor cells. The treatment of the strips with 20 μg/mL BFA for 6 hours completely abolishes the relaxation induced by bradykinin in the presence of 10mM indomethacin and 30 μM L-NOARG. The treatment with 20 μg/mL of this compound substantially abolishes the bradykinin-induced decreases in [Ca²⁺]_i and tension in the range of concentrations between 1 nM and 1 mM. It has no effect on the [Ca²⁺]_i elevation in endothelial cells induced by bradykinin or substance P. Addition of the fungal metabolite does not affect the spontaneous phospholipid-dependent GTPS binding to myr-rARF1 but totally abolishs the retinal isotonic extract (RIE)-catalyzed exchange, with half-maximal inhibition at 2 μM. It prevents a wide variety of membrane traffic pathways and inhibits an ADP-ribosylation factor-specific guanine nucleotide exchange activity present in Golgi membranes or in brain cytosol. The complete prevention by this compound strongly suggests that the retinal extract contains an ARF-specific guanine nucleotide exchange factor. Retinal isotonic extract (RIE)-catalyzed GTPS release from both ADP-ribosylation factors (ARFs) is only partly inhibited by BFA, even at 300 μM. It induces fusion of the Golgi apparatus with the ER and abolishes the inhibitory effect of the CERT inhibitor HPA-12. Treatment with this compound, which induces fusion of the Golgi apparatus and the ER, rescues the limonoid-induced prevention of sphingomyelin biosynthesis. Its treatment of CHO cells causes a 2 to 3 fold increase in sphingomyelin synthesis. Apart from B-CLL cells, BFA reportedly causes apoptosis in multiple myeloma (U266, NCI-H929), Jurkat, HeLa, leukaemia (HL60, K562, BJAB), colon (HT-29) and prostate, as well as adenoid cystic sarcoma cells. The administration of 25 ng/mL of this compound completely blocks growth of HF4.9 and HF28RA cells, whereas higher doses (75 ng/mL) are required to achieve the same effect in HF1A3 cells. Cell proliferation is inhibited within 24 hours in a dose-dependent manner and, depending on the cell line, almost complete cessation of ³H-thymdine incorporation is observed at 50-75 ng/mL (26%, 76%, 87% inhibition at 50 ng/ml and 75%, 87%, 92% inhibition at 75 ng/mL for HF1A3, HF4.9 and HF28RA cells respectively. BFA-induced cell killing is in a dose-dependent manner using YO-PRO 1/PI assay. It could improve the HDR(homology-directed repair) efficiency and is an enhancer of CRISPR-mediated HDR.
In vivo	Brefeldin A (BFA), a lactone antibiotic and specific inhibitor of protein trafficking, blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus.
References	[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/