Brefeldin A | BFA | Protein Transport Inhibitor | AmBeed-信号通路专用抑制剂

Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

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产品名称	ATPase ↓ ↑	纯度
(-)-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. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Autophagy ↓ ↑	其他靶点	纯度
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. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cell Line neutrophils AML12 cells PFHR-9 WT cells T24 bladder cancer cells COS7 cells HeLa cells porcine intestinal epithelial cells (IPEC-1) J82 T24 CIK cells IC21 murine macrophages	Concentration	Treated Time	Description	References
neutrophils	3 μg/ml	4 h	BFA treatment reversed the upregulation of surface CD9 and CD47 expression by OTUD1 deficiency upon LPS stimulation, indicating that BFA limits OTUD1-deficient neutrophil secretion by blocking protein transport signaling.	Adv Sci (Weinh). 2023 Oct;10(30):e2303207.
AML12 cells	10 μM	24 h	To evaluate the effect of Brefeldin A on XOR release, results showed that Brefeldin A did not alter XOR release	Redox Biol. 2023 Nov;67:102866.
PFHR-9 WT cells	5 μM	12 h	Validate the effect of Brefeldin A on inhibiting the secretory pathway of PXDN, results showed that Brefeldin A inhibited the secretion of PXDN.	Redox Biol. 2022 Aug;54:102385.
T24 bladder cancer cells	10-40 nM	24 h	To investigate the effects of BFA on ER morphology and cell biomechanics in T24 bladder cancer cells. Results showed that BFA significantly altered the subcellular distribution of the ER and was associated with cytoskeletal rearrangement.	Cell Commun Signal. 2023 Oct 30;21(1):307.
COS7 cells	5 µg/ml	50 min	To investigate the effect of BFA treatment on Golgi structure, it was found that BFA treatment causes Golgi dispersion.	J Cell Biol. 2024 Dec 2;223(12):e202311189.
HeLa cells	5 µg/ml	1 hour	To investigate the effect of VPS13B loss on Golgi structure, it was found that the absence of VPS13B delays Golgi recovery.	J Cell Biol. 2024 Dec 2;223(12):e202311189.
porcine intestinal epithelial cells (IPEC-1)	0.1 µM	12 h	To investigate the effect of BFA on apoptosis and intestinal barrier function in IPEC-1 cells, results showed that BFA treatment led to increased apoptosis and upregulation of proteins involved in ER stress signaling, while inducing dysfunction in the intestinal epithelial barrier.	Anim Nutr. 2022 Mar;8(1):1-9.
J82	0.081 μM	72 h	To evaluate the antiproliferative activity of CHNQD-01281 on J82 cells, the results showed that CHNQD-01281 significantly inhibited the proliferation of J82 cells with an IC50 value of 0.081 μM	Mar Life Sci Technol. 2024 Aug 5;6(3):502-514.
T24	0.079 μM	72 h	To evaluate the antiproliferative activity of CHNQD-01281 on T24 cells, the results showed that CHNQD-01281 significantly inhibited the proliferation of T24 cells with an IC50 value of 0.079 μM	Mar Life Sci Technol. 2024 Aug 5;6(3):502-514.
CIK cells	0.5 mg/ml, 2.5 mg/ml, 10 mg/ml	1 hour, 12 h, 24 h	To investigate the effect of BFA on GCRV replication and infection. Results showed that BFA treatment significantly inhibited GCRV replication and infection, and reduced the number of viral inclusion bodies.	Front Immunol. 2022 Aug 26;13:956587.
IC21 murine macrophages	5 µg/ml	1 hour	Brefeldin A was used to block protein secretion from the ER to the Golgi apparatus. The experimental results showed that Brefeldin A treatment did not lead to the accumulation of IL-36γ within the cells, indicating that IL-36γ is not secreted through the conventional secretory pathway.	Front Immunol. 2022 Aug 18;13:979749.

Species Mice Zebrafish Nude mice	Animal Model Experimental periodontitis model Fam177a1a;fam177a1b DKO;vps13b crispant T24 xenograft mouse model	Administration	Dosage	Frequency	Description	References
Mice	Experimental periodontitis model	Gingival injection	100 μg/ml	Injected on day 1 and day 3	GelMA/BFA significantly suppressed neutrophil recruitment to the gingiva in Otud1─/─mice and effectively ameliorated periodontal inflammation and alveolar bone destruction.	Adv Sci (Weinh). 2023 Oct;10(30):e2303207.
Zebrafish	Fam177a1a;fam177a1b DKO;vps13b crispant	Immersion	0.8 µg/ml	From 6 hpf to 25 hpf	To investigate the effect of BFA treatment on zebrafish development, it was found that BFA treatment reduces zebrafish body length.	J Cell Biol. 2024 Dec 2;223(12):e202311189.
Nude mice	T24 xenograft mouse model	Intraperitoneal injection	30 mg/kg	Once daily for two weeks	To evaluate the antitumor effect of CHNQD-01281 in the T24 xenograft mouse model, the results showed that CHNQD-01281 significantly suppressed tumor growth with a tumor growth inhibition rate of 52.63%	Mar Life Sci Technol. 2024 Aug 5;6(3):502-514.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01742364	-		Completed	-	-
NCT01742364	Tuberculosis	Not Applicable	Completed	-	South Africa ... 展开 >> SATVI, University of Cape Town Cape Town, South Africa, 7925 收起 <<
NCT03044509	-		Recruiting	December 2019	Switzerland ... 展开 >> Kantonspital Aarau Recruiting Aarau, Switzerland, 5001 Contact: Sara Bernhard-Stirnemann, Dr med +41628384192 sara.bernhard@ksa.ch Kinderspital Basel Recruiting Basel, Switzerland, 4031 Contact: Marina Beaufils-Hugot, PhD +41617042953 marina.beaufils-hugot@ukbb.ch Contact: Noemi Meier, Master +41617042947 noemi.meier@ukbb.ch Principal Investigator: Nicole Ritz, PD Dr med Sub-Investigator: Ines Mack, Dr med Sub-Investigator: Anja Jochmann, Dr med Sub-Investigator: Daniel Trachsel, PD Dr med Ospedale Regionale di Bellinzona Recruiting Bellinzona, Switzerland, 6500 Contact: Lisa Kottanattu, Dr med +41918118538 lisa.kottanattu@eoc.ch Inselspital Bern Recruiting Bern, Switzerland, 3010 Contact: Andrea Duppenthaler, Dr. med. +41316329414 andrea.duppenthaler@insel.ch Hôpital des enfants - HUG Recruiting Genève, Switzerland, 1205 Contact: Anne Mornand, Dr. med. +41223724579 anne.mornand@hcuge.ch Sub-Investigator: Marie Rohr, Dr. med. Kinserspital Luzern Recruiting Luzern, Switzerland, 6016 Contact: Michael Buettcher, Dr med +41412056657 michael.buettcher@luks.ch Kinderspital St Gallen Recruiting St. Gallen, Switzerland, 9006 Contact: Jürg Barben, Prof Dr med +41712437111 juerg.barben@kispisg.ch Sub-Investigator: Christian Kahlert, Dr med Kinderklinik Zürich Recruiting Zürich, Switzerland, 8032 Contact: Christoph Berger, Prof Dr med +41442667840 christoph.berger@kispi.uzh.ch Sub-Investigator: Christa Relly, Dr med 收起 <<

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

3T3-L1	5 μg/ml	Function Assay	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	5 μg/ml	Function Assay	30 min	recapitulates insulin action with respect to regulating Akt activity and AS160 phosphorylation	24843827
3T3-L1	5 μg/ml	Function Assay	30 min	causes reversible redistribution of GLUT4	24843827
3T3-L1	5 μg/ml	Function Assay	1 h	causes redistribution of GLUT4 but not increase in glucose uptake	24843827
3T3-L1	5 μg/ml	Function Assay	1 h	causes phosphorylation of the FoxO1 transcription factor	24843827
A172	10 μg/ml	Function Assay	4 h	results in the retrograde transport of fluorescent granules	25239507
A549		Growth Inhibition Assay		IC50=0.04 μg/ml	23793342
ADF	10 μM	Function Assay	16 h	inhibits the ZnCl2-induced translocation of CRT	24228232
ADF	10 μM	Function Assay	6 h	impairs the DC activation	24228232
BAECs	5 μg/ml	Function Assay	0-4 h	induces the rapid dephosphorylation of eNOS at Ser1179	24085225
C2C12	1 μg/ml	Function Assay	1 h	abolishes cytokine release from C2C12 myotubes	26291279
Caco-2	2.5 μM	Function Assay	30 min	attenuates the TGF-β1-mediated increase in SERT function	25954931
Colo 205	0-5 μg/mL	Growth Inhibition Assay	48 h	inhibits cell growth in suspension cultures with an estimated IC50 of ~15 ng/mL	23973996
Colo 205	0.012-0.025 μg/mL	Function Assay	14 d	reduces the clonogenicity of Colo 205 CSCs	23973996
Colo 205	0.1 μg/mL	Apoptosis Assay	0-24 h	induces apoptosis of Colo 205 cells in suspension cultures	23973996
Colo 205	0.015 μg/mL	Function Assay	24 h	induces the expression of ER stress-related genes	23973996
Colo 205	0.015 μg/mL	Function Assay	24 h	inhibits the activity of MMPs	23973996
COS	1 μg/ml	Function Assay	3 h	completely disperses the AP-1 signal	25915900
COS-1	5 µg/ml	Function Assay	24 h	restricts localization of NB in the perinuclear region	24671751
DF1	1 μM	Function Assay	48 h	disperses the exogenous CSGalNAcT2 protein	25807054
FRT	5 μg/ml	Function Assay	2 h	blocks trafficking through the Golgi complex by inhibiting ER-to-Golgi transport	25767115
FRT	5 μg/ml	Function Assay	2 h	prevents the increase in cleaved α subunits when [Na+]i was reduced	25767115
H1299	10 μg/ml	Function Assay	24 h	induces autophagy	25388970
H838-KDLKB1	30 ng/ml	Function Assay	12/18 h	increases the protein levels of BiP	25011082
H838-KDLKB1	30 ng/ml	Function Assay	12/18 h	increases the levels of phosphorylated eIF2α (phospho-eIF2α)	25011082
H838-LKB1	30 ng/ml	Function Assay	12/18 h	increases the protein levels of BiP	25011082
HEK293	5 μg/ml	Function Assay	12 h	abolishes CMA-induced CRELD2 secretion	24687431
HEK293/hERG	10 μM	Function Assay	1 h	results in a time-dependent reduction mature hERG protein	25218469
HEK293/tau	5 μM	Function Assay	1/2/4 h	induces Golgi fragmentation	24368089
HEK293/tau	5 μM	Function Assay	3 h	induces tau hyperphosphorylation	24368089
HeLa	200 ng/ml	Function Assay	3 h	induces the artificial break-up of the Golgi complex	25948586
HeLa	5 μg/ml	Function Assay	3 h	causes nuclear exclusion of the FoxO1 transcription factor and decreases transcription of FoxO1-regulated genes	24843827
HeLa	2 μM	Function Assay	2 h	attenuates the TNF-induced secretion of IL-15	23950892
HEMC-1	0.1 µg/ml	Function Assay	24 h	causes a higher inhibitory effect on exocytosis than nocodazole	25972759
HepG2	1 µM	Function Assay	24 h	decreases the level of PXR mRNA	25616597
HepG2	1μg/mL	Function Assay	3–24 h	increases the level of APE1 in a time-dependent manner	25026174
HepG2		Growth Inhibition Assay		IC50<0.001 μg/ml	23793342
HFS	0-1 μg/ml	Function Assay	24 h	GLTP expression reaches a plateau at concentrations as low as 0.01 µg/ml	23894633
HFS	0.01 µg/ml	Function Assay	24 h	increases the expression of glycosphingolipid synthase genes at 6 h	23894633
HL-60		Growth Inhibition Assay		IC50<0.001 μg/ml	23793342
Huh7	5 μg/ml	Function Assay	4 h	abolishes the secretion of intracellular ApoB	24100140
Huh7	5 μg/ml	Function Assay	1 h	causes a significant increase in ApoB-crescents	24100140
Huh7	5–10 ng/ml	Function Assay	12 h	increases ApoB-crescents without inhibiting secretion	24100140
Huh-7	1μg/mL	Function Assay	3–24 h	increases the level of APE1 in a time-dependent manner	25026174
HUVEC	10 μM	Function Assay	1 h	abolishes hypoxia-induced release of ATP from apical and basolateral surfaces	25956988
HUVEC	10 μM	Function Assay	1 h	increases the number and intensity of fluorescent areas especially in perinuclear space	25956988
IBRS2	5 μg/ml	Function Assay	0.5 h	disrupts the ERGIC and Golgi	23963534
IBRS2	5 μg/ml	Function Assay	0.5 h	enhances FMDV infection	23963534
iPSC-CMs	500 ng/ml	Function Assay	48 h	increases the intensity of the higher mobility LAMPs at the cost of the lower mobility species	25488666
KMS-6	1 μM	Function Assay	24 h	exhibits half the secretion of galanin-LI as did the control	25229126
LOVO		Growth Inhibition Assay		IC50=0.12 μg/ml	23793342
Macrophages	71 µM	Function Assay	6 h	inhibits lunasin internalization	24039740
MDA-MB-231	0–50 μg/mL	Cell Viability Assay	48 h	EC50 = 0.016 µg/mL	25356567
MDA-MB-231	0.1 μg/mL	Apoptosis Assay	4 h	induces apoptosis	25356567
MDA-MB-231	0.01/0.05 μg/mL	Growth Inhibition Assay	24 h	increases the fraction of sub-G1 cell debris	25356567
MDA-MB-231	0.05–1 μg/mL	Apoptosis Assay	24 h	induces PARP (poly ADP-ribose polymerase-1) cleavage	25356567
MDA-MB-231	0–50 μg/mL	Function Assay	24 h	inhibits the formation of 3D and 2D colonies	25356567
MDA-MB-435		Growth Inhibition Assay		IC50<0.001 μg/ml	23793342
MDMs	10 μg/ml	Apoptosis Assay	12/15 h	induces apoptosis	24556695
MEC	1 μM	Function Assay	1.5 h	causes a dramatic decrease in the surface VEGFR2	25228815
MEFs VAMP7 KO	5 μM	Function Assay	20 min	causes resident enzymes such as NAGT-GFP, to diffuse back to the ER	26196023
MEFs WT	5 μM	Function Assay	20 min	causes resident enzymes such as NAGT-GFP, to diffuse back to the ER	26196023
MKN45		Growth Inhibition Assay		IC50<0.001 μg/ml	23793342
nHDFs	1 μM	Function Assay	2 h	prevents the assembly of cytosolic coat proteins onto Golgi membranes	25772616
NRK	200 ng/ml	Function Assay	4 h	rescues mitotic progression	25948586
OB-6	2.7 μM	Apoptosis Assay	48 h	induces apoptosis	25532480
OVCAR-3	1–15 μM	Growth Inhibition Assay	24 h	induces a loss of cell viability dose dependently	23826964
OVCAR-3	1–15 μM	Function Assay	24 h	induces nuclear damage	23826964
OVCAR-3	1-10 μM	Apoptosis Assay	4 h	induces the activation of apoptosis-related proteins	23826964
OVCAR-3	10 μM	Apoptosis Assay	24 h	induces activation of caspases	23826964
OVCAR-3	1–10 μM	Function Assay	24 h	induces disruption of the mitochondrial transmembrane potential	23826964
OVCAR-3	1–10 μM	Function Assay	24 h	induces formation of reactive oxygen species	23826964
OVCAR-3	1–10 μM	Function Assay	24 h	inhibits cell adhesion and migration	23826964
PC12	2 μM	Function Assay	1 h	inhibits the L-DOPA (20 μM)-induced transient ERK1/2 phosphorylation	26363191
PEXEL-Nluc	5 mg/mL	Function Assay	6 h	causes an increase in reporter activity in the parasite	25392998
PMHs	10–20 μg/ml	Function Assay	24 h	induced ER stress	24407242
PMHs	10–20 μg/ml	Apoptosis Assay	24 h	increases cell death	24407242
PRP	10 μM	Function Assay		abrogates SDF-1α-mediated CXCR7 externalization	24668750
RAW264.7	4 μM	Apoptosis Assay	48 h	attenuates the inhibition of ox-LDL-induced apoptosis and the facilitation of cholesterol efflux by Ac-hE-18A-NH2	24639032
RBE4	2 μM	Apoptosis Assay	3–24 h	induces apoptosis time dependently	25128025
RBE4	2 μM	Function Assay	3–24 h	increases the XBP1 protein levels after 3 and 6 h of treatment	25128025
RBE4	2 μM	Function Assay	3–24 h	increases active caspase-12 in a time-dependent manner	25128025
RBE4	2 μM	Function Assay	3–24 h	increases the levels of ROS time-dependently	25128025
RBE4	2 μM	Function Assay	3–24 h	induces a delayed depletion of the ER Ca2+ content at 6 h of incubation significantly	25128025
RBE4	2 μM	Function Assay	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
RKO-HIPK2i	10 μM	Function Assay	16 h	inhibits the ZnCl2-induced translocation of CRT	24228232
SMCs	10 µg/ml	Function Assay	0-12 h	shows a trend towards a higher concentration of the ER/SR network in the perinuclear area	26172080
SMCs	10 µg/ml	Function Assay	0-12 h	causes a transient Ca2+ release from the ER/SR	26172080
SMCs	1μg/mL	Function Assay	3 h	accumulates CNPY2 protein in the ER compartment and no longer co-localized with the Golgi marker	25589425
SP-Nluc	5 mg/mL	Function Assay	6 h	causes an increase in reporter activity in the parasite	25392998
U373	10 μM	Function Assay	16 h	inhibits the ZnCl2-induced translocation of CRT	24228232

靶点	ATPase ATPase (HCT 116), IC50:0.2 μM
描述	Brefeldin A is a fungal lactone antibiotic produced by Penicillium brefeldianum usually used as a protein trafficking/secretion inhibitor in mammalian and other eukaryotic cells, without significant effect on protein synthesis. The main target of Brefeldin A may be Arf1, which is important to formation of protein transport vesicles^[1]^[2]^[3]. Brefeldin A could induce the rapid redistribution of the ll0-kD protein and the movement of Golgi membrane into the ER within 15min at 2μg/ml in semipermeable cells^[4]. Brefeldin A could induce a wide variety of human cancer cells to differentiation and apoptosis. It exhibited cytotoxicity to HCT 116 cells with IC50 value of 0.2μM, as well as induced DNA fragmentation and apoptotic morphological changes with IC50 values of 0.11 and 0.36 μM, respectively^[5]. Brefeldin A combined with L755507 could improve the HDR efficiency, and exhibit enhanced insertion efficiency by 2-fold, with maximal effect at 0.1 μM^[6].
作用机制	Brefeldin A inhibits protein trafficking and secretion by interfering with the function of the Golgi apparatus, which may due to the disruption of transport vesicle formation dependent on the assembly of the COPI coat by Arf1-GTP.^[1]^[2]^[3]

Dose	Mice: 26.3 mg/kg^[7] (i.v.), LD50 = 250 mg/kg^[8] (i.p.)
Administration	i.v., i.p.

CAS号	20350-15-6
分子式	C₁₆H₂₄O₄
分子量	280.36
SMILES Code	O[C@@H]1C[C@]2([H])[C@@](/C=C/CCC[C@H](C)OC(/C=C/[C@H]2O)=O)([H])C1
MDL No.	MFCD00083258

别名	BFA; Decumbin; Bredfeldin A; Synergisidin; NSC 244390; NSC 107456; NSC 89671; NSC 56310; Nectrolide; Ascotoxin; Cyanein
运输	蓝冰

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