来普霉素B
基本信息
产品名称 | 来普霉素B |
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英文名称 | Leptomycin B |
别名 | 细霉素B |
英文别名 | Mantuamycin;LMB;Elactocin;Antibiotic CI 940;Antibiotic CL 1957A;NSC 364372 |
规格或纯度 | 98% |
运输条件 | 超低温冰袋运输 |
生化机理 | Leptomycin B is an unsaturated, branched-chain fatty acid, and is an important tool in the study of nuclear export. It is a specific inhibitor of proteins containing nuclear export signal. It inhibits nucleo-cytoplasmic translocation of molecules such as the HIV-1 Rev protein and Rev-dependent export of mRNA. The addition of very small amounts to fibroblasts causes accumulation of MEK in the nucleus. Other proteins that are influenced by leptomycin B are actin, c-Abl, cyclin B1, MDM2/p53, IκB, MPF, and PKA. The sμggested inhibition mechanism involves the direct binding of leptomycin B to CRM1, which blocks the binding of CRM1 to proteins containing the nuclear export signal, via the interaction with cysteine residue in CRM1 control conserved region.Potent inhibitor of CRM-1-mediated (exportin-1) nuclear export. Displays antibiotic, antifungal, and antitumor properties and blocks the cell cycle at G 1 and G 2 phases. |
一般描述
Leptomycin B is an anti-fungal antibiotic, anti-tumor cytotoxin that inhibits CRM1-dependent, NES-dependent nucleo-cytoplasmic translocation (nuclear export inhibitor). NES containing proteins include HIV-1 REV; actin, c-Abl, cyclin B1, MDM2/p53, IB, MPF, PKA and MEK.Leptomycin B is a potent and specific nuclear export inhibitor. Leptomycin B alkylates and inhibits CRM1 (chromosomal region maintenance)/exportin 1, a protein required for nuclear export of proteins containing a nuclear export sequence (NES). In addition to antifungal and antibacterial activities, Leptomycin B blocks the cell cycle and is a potent anti-tumor agent. At low nM concentrations, Leptomycin B blocks the nuclear export of many proteins including HIV-1 Rev, MAPK/ERK, and NF-κB/IκB, and it stabilizes the expression of p53. Leptomycin B also inhibits the export and translation of many RNAs, including COX-2 and c-Fos mRNAs, by inhibiting export of ribonucleoproteins.
Leptomycin B is an anti-fungal antibiotic, anti-tumor cytotoxin that inhibits CRM1-dependent, NES-dependent nucleo-cytoplasmic translocation (nuclear export inhibitor). NES containing proteins include HIV-1 REV; actin, c-Abl, cyclin B1, MDM2/p53, IB, MPF, PKA and MEK.
Leptomycin B is a potent and specific nuclear export inhibitor. Leptomycin B alkylates and inhibits CRM1 (chromosomal region maintenance)/exportin 1, a protein required for nuclear export of proteins containing a nuclear export sequence (NES). In addition to antifungal and antibacterial activities, Leptomycin B blocks the cell cycle and is a potent anti-tumor agent. At low nM concentrations, Leptomycin B blocks the nuclear export of many proteins including HIV-1 Rev, MAPK/ERK, and NF-κB/IκB, and it stabilizes the expression of p53. Leptomycin B also inhibits the export and translation of many RNAs, including COX-2 and c-Fos mRNAs, by inhibiting export of ribonucleoproteins.
相关属性
CAS编号 | 87081-35-4 |
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敏感性 | 对湿度敏感,对光敏感 |
溶解性 | Soluble in ethanol or methanol. Ethanol is recommended. Unstable in DMSO |
储存温度 | 避光,-20°C储存,充氩 |
MDL号 | MFCD06795848 |
密度 | 1.072 |
分子量 | 540.73 |
分子式 | C33H48O6 |
品牌 | Jinpan |
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PubChem CID | 6917907 |