CAS: 80890-47-7; Concanamycin A

该化合物是一种强效大型滑动抗生素和真空型H+-ATPase(V-ATPase)抑制剂,广泛用于生化化学和药理研究,其主要行动机制包括选择性抑制V-ATPase,干扰细胞内PH调节和输卵器贩运.这种特性使它成为研究淋巴功能,自发和内分泌途径的宝贵工具.Concanamy A具有很高的特性和效力,对哺乳动物和微生物V-ATPases都进行了示范活动,其有机溶剂的稳定性和溶性促进了实验应用.研究人员利用Concanamycin A调查离子传输机制,有机酸化及相关细胞过程,有助于细胞生物学和药物发现的进步.

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    专利号:WO-9958147-A1
    优先权日:1998-05-08
    标 题 :APOPTOSIS OF NAIVE HUMAN NK CELLS BY CROSSLINKING OF THEIR FcγRIIIa MOLECULES WIHT A RAT IgG2b (LO-CD2a/BTI-322) OR ITS IgG1 HUMANIZED MONOCLONAL ANTIBODY
    发明人:BAZIN HERVE; LATINNE DOMINIQUE
    权利人:UNIV CATHOLIQUE LOUVAIN
    摘要:Although the mechanism of induction of apoptosis through antibody dependent cellular cytotoxicity (ADCC) mediated by NK cells is well understood, little is known about the fate of the reactive NK cells. Nevertheless, it has been shown that NK cells previously activated by IL-2, but not naive NK cells, died by apoptosis after FcγRIIIa crosslinking, or after engagement in cytolytic functions. It is demonstrated that apoptosis of naive NK cells is also observed after stimulation with a rat IgG2b anti CD2 mAb (LO-CD2a/BTI-322) or anti HLAI (LO-HLA-1)mAb. The NK apoptosis is rapid (within minutes), Fas-ligand and mRNA synthesis independent and does not require a cell contact. The intracellular mechanism of NK cell apoptosis is calcium, PKC and PLA2 dependent but calcineurin and P13 kinase independent. We suggest that NK cell apoptosis results from the crosslinking on the same cell surface of CD2 or HLA-I molecules and FcγRIIIa that exhibits a high affinity for the rat IgG2b isotype. The clinical application of these experiments are discussed.

    专利号:US-6692743-B1
    优先权日:1998-05-08
    标 题:Apoptosis of naive human NK cells by crosslinking of their FcγRIIIa molecules with a rat IgG2b (LO-CD2a/BTI-322) or its IgG1 humanized monoclonal antibody
    发明人:BAZIN HERVE; LATINNE DOMINIQUE
    权利人:UNIV CATHOLIQUE LOUVAIN
    摘要:Although the mechanism of induction of apoptosis through antibody dependent cellular cytotoxicity (ADCC) mediated by NK cells is well understood, little is known about the fate of the reactive NK cells. Nevertheless, it has been shown that NK cells previously activated by IL-2, but not naive NK cells, died by apoptosis after FcγRIIIa crosslinking, or after engagement in cytolytic functions. It is demonstrated that apoptosis of naive NK cells is also observed after stimulation with a rat IgG2 b anti CD2 mAb (LO-CD2 a /BTI-322) or anti HLAI (LO-HLA-1)mAb. The NK apoptosis is rapid (within minutes), Fas-ligand and mRNA synthesis independent and does not require a cell contact. The intracellular mechanism of NK cell apoptosis is calcium, PKC and PLA2 dependent but calcineurin and P13 kinase independent. We suggest that NK cell apoptosis results from the crosslinking on the same cell surface of CD2 or HLA-I molecules and FcγRIIIa that exhibits a high affinity for the rat IgG2 b isotype. The clinical application of these experiments are discussed.

    专利号:EP-0635577-B1
    优先权日:1993-07-23
    标 题 :Screen for inhibitors of melanin biosynthesis
    发明人:BRINDLE FRANCES HARRIET ELIZAB; FROELIGER EUNICE HARRIET
    权利人:BASF AG
    摘要:A method for the identification of agents that inhibit melanin biosynthesis involves the incubation of test samples in cultures of a fungus that produces melanin. Observation of altered pigmentation in the culture or culture area containing test sample indicates inhibition of melanin biosynthesis. Preferred cultures for the screen contain a fungus that pigments in the light or the dark such as Cladosporium cucumerinum. Preferred embodiments employ test samples on disks or in wells in solidified cultures and a known melanin synthesis inhibitor as a positive control which is compared to the test sample by simple visual inspection.

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    1: Zhang CS, Li M, Zong Y, Lin SC. Determining AMPK Activation via the Lysosomal v-ATPase-Ragulator-AXIN/LKB1 Axis. Methods Mol Biol. 2018;1732:393-411. doi: 10.1007/978-1-4939-7598-3_25. doi: 10.1016/j.bbagen.2017.12.006. Epub 2017 Dec 16. doi: 10.1016/j.bbrc.2017.12.077. Epub 2017 Dec 15. doi: 10.1093/jxb/erx372. doi: 10.1007/978-1-4939-7389-7_19. doi: 10.1242/bio.028837.
    8: Gilmartin AA, Ralston KS, Petri WA Jr. Inhibition of Amebic Lysosomal Acidification Blocks Amebic Trogocytosis and Cell Killing. MBio. 2017 Aug 29;8(4). pii: e01187-17. doi: 10.1128/mBio.01187-17.
    9: Uhlman A, Folkers K, Liston J, Pancholi H, Hinton A. Effects of Vacuolar H(+)-ATPase Inhibition on Activation of Cathepsin B and Cathepsin L Secreted from MDA-MB231 Breast Cancer Cells. Cancer Microenviron. 2017 Dec;10(1-3):49-56. doi: 10.1007/s12307-017-0196-7. Epub 2017 Aug 2.

    合成参考文献


    摘要:United States Patent Document., #4076802
    参考文献:10.1006/cryo.1999.2163
    摘要:Edashige K, Asano A, An TZ, Kasai M. Restoration of resistance to osmotic swelling of vitrified mouse embryos by short-term culture. Cryobiology. 1999 Jun;38(4):273–80. doi: 10.1006/cryo.1999.2163.
    参考文献:10.1186/1471-213x-4-7
    摘要:Malchow D, Lusche DF, Schlatterer C. A link of Ca2+ to cAMP oscillations in Dictyostelium: the calmodulin antagonist W-7 potentiates cAMP relay and transiently inhibits the acidic Ca2+-store. BMC Developmental Biology. 2004 May 17;4(1):7. doi: 10.1186/1471-213x-4-7.
    参考文献:10.1016/j.bbamem.2004.03.003
    摘要:Páli T, Dixon N, Kee TP, Marsh D. Incorporation of the V-ATPase inhibitors concanamycin and indole pentadiene in lipid membranes. Spin-label EPR studies. Biochimica et Biophysica Acta (BBA) - Biomembranes. 2004 May;1663(1-2):14–8. doi: 10.1016/j.bbamem.2004.03.003.
    参考文献:10.1016/j.bbrc.2004.04.180|10.1016/s0006-291x(04)00948-9
    摘要:Caron NJ, Quenneville SP, Tremblay JP. Endosome disruption enhances the functional nuclear delivery of Tat-fusion proteins. Biochemical and Biophysical Research Communications. 2004 Jun;319(1):12–20. doi: 10.1016/j.bbrc.2004.04.180.
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