Brefeldin A inhibits protein translocation from the endoplasmic reticulum (ER) to the Golgi apparatus reversibly, can be used to induce autophagy in mammalian cells.
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产品名称 | ATPase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
(-)-Blebbistatin | 99%+ | ||||||||||||||||||
PF 03716556 |
++++
H+/K+-ATPase, pIC50: ~6.5 |
98% | |||||||||||||||||
Esomeprazole sodium | ✔ | 98% | |||||||||||||||||
BTB06584 | ✔ | 98% | |||||||||||||||||
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 |
99% | |||||||||||||||||
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 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
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。 |
靶点 |
|
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] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 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 |
Dose | Mice: 26.3 mg/kg[7] (i.v.), LD50 = 250 mg/kg[8] (i.p.) |
Administration | i.v., i.p. |
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 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.57mL 0.71mL 0.36mL |
17.83mL 3.57mL 1.78mL |
35.67mL 7.13mL 3.57mL |
CAS号 | 20350-15-6 |
分子式 | C16H24O4 |
分子量 | 280.359 |
别名 | BFA;Decumbin;Bredfeldin A;Synergisidin;NSC 244390;NSC 107456;NSC 89671;NSC 56310;Nectrolide;Ascotoxin;Cyanein |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(374.52 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 10 mg/mL(35.67 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 |
动物实验配方 |