| Description | Concanamycin A (Folimycin), a polycyclic lactone antibiotic, is a selective inhibitor of vacuolar H+-ATPase (V-ATPase) and lysosomal acidification, and can be used to study inflammation.Concanamycin A enhances the immune clearance of infected progenitor cells by cytotoxic T lymphocytes, and inhibits Nef et al. from different branches of HIV and simian immunodeficiency virus. Concanamycin A enhances immune clearance of cytotoxic T lymphocytes from infected progenitor cells, inhibits the Nef allele from different branches of HIV and simian immunodeficiency virus, and can be used to study HIV infection. |
| In vitro | 在 CD8+ 细胞毒性 T 淋巴细胞（CTLs）中，Concanamycin A（100 nM；0、4、8、12、16、20小时）在20小时内诱导了快速细胞死亡，而不是凋亡，且未观察到细胞核浓缩现象[2]。 |
| In vivo | 在野生型小鼠中，Concanamycin A（15 mg/kg；静脉注射，在处死前 0、10 或 24 小时进行）导致显著的肝损伤，表现为血清转氨酶水平升高、炎症细胞浸润、肝细胞凋亡以及在给药后 10 小时和 24 小时内包括白细胞介素4（IL4）和干扰素γ（IFNγ）在内的多种细胞因子表达增加[5]。 |
| Synonyms | Folimycin, Concanamycin, X 4357B, Antibiotic X 4357B |
| molecular weight | 866.09 |
| Molecular formula | C46H75NO14 |
| CAS | 80890-47-7 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 8 mg/mL (9.24 mM), Sonication is recommended. Methanol: 8 mg/mL (9.24 mM), Sonication and heating are recommended. |
| References | 1. Vaněk, Z., et al. Immunomodulators isolated from microorganisms. Folia Microbiol. 1991. 36:99–111. 2. Togashi K, et al. Concanamycin A, a vacuolar type H(+)-ATPase inhibitor, induces cell death in activated CD8(+) CTL. Cytotechnology. 1997 Nov;25(1-3):127-35. 3. Eswarappa SM, et al. Folimycin (concanamycin A) inhibits LPS-induced nitric oxide production and reduces surface localization of TLR4 in murine macrophages. Innate Immun. 2008 Feb;14(1):13-24. 4. Hines IN, et al. Impaired T cell-mediated hepatitis in peroxisome proliferator activated receptor alpha (PPARα)-deficient mice. Biol Res. 2018 Feb 15;51(1):5. 5. Woo JT, et al. Isolation, characterization and biological activities of concanamycins as inhibitors of lysosomal acidification. J Antibiot (Tokyo). 1992 Jul;45(7):1108-16. |