Leptomycin B
- CAS No.
- 87081-35-4
- Chemical Name:
- Leptomycin B
- Synonyms
- Lepomycin B;Leprimycin B;LEPTOMYCIN B;antibioticci940;antibioticcl1957a;Leptomycin B solutio;Leptomycin B (CI 940;LeptoMycin B 1% soluton;Leptomycin B (0.2mg/ml);InSolution? Leptomycin B,
- CBNumber:
- CB9500811
- Molecular Formula:
- C33H48O6
- Molecular Weight:
- 540.73
- MOL File:
- 87081-35-4.mol
- Modify Date:
- 2023/9/4 15:51:00
| Melting point | 41-44°, with prior softening (Hokanson) |
|---|---|
| alpha | D -24.5° (c = 0.70 in MeOH); D23 -157 ° (c = 0.7% in chloroform) |
| Boiling point | 725.8±60.0 °C(Predicted) |
| Density | 1.072±0.06 g/cm3(Predicted) |
| Flash point | 11°(52°F) |
| storage temp. | −20°C |
| solubility | Supplied in solution in ethanol (1 mg/ml). Further dilutions may be made with either ethanol or DMSO. |
| form | Liquid |
| pka | 5.10±0.33(Predicted) |
| color | White to off-white |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions or dilutions in DMSO are not stable. Solutions should be made fresh and used within one working day. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS02,GHS06,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H225-H301+H311+H331-H370 | |||||||||
| Precautionary statements | P210-P280-P301+P310+P330-P302+P352+P312-P304+P340+P311 | |||||||||
| Hazard Codes | F,T | |||||||||
| Risk Statements | 23/25-36/38-39/23/24/25-23/24/25-11 | |||||||||
| Safety Statements | 7-16-24-33-45-36/37 | |||||||||
| RIDADR | UN 1230 3/PG 2 | |||||||||
| WGK Germany | 3 | |||||||||
| HazardClass | 3 | |||||||||
| HS Code | 29419090 | |||||||||
| NFPA 704 |
|
Leptomycin B price More Price(2)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | L2913 | Leptomycin B solution from Streptomyces sp. ≥95% (HPLC), Supplied in methanol: water (7:3) | 87081-35-4 | 0.5μG | ₹6440.88 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | L2913 | Leptomycin B solution from Streptomyces sp. ≥95% (HPLC), Supplied in methanol: water (7:3) | 87081-35-4 | 5μG | ₹40431.38 | 2022-06-14 | Buy |
Leptomycin B Chemical Properties,Uses,Production
Uses
Leptomycin B is the dominant and most studied member of the leptomycin class, isolated from selected Streptomyces strains. Leptomycin B is a nanomolar active and specific nuclear export inhibitor. Its target is CRM1/exportin1, a protein in the nuclear export sequence (NES). Proteins affected include c-Abl, cyclin B1, HIV-1 Rev, IκB, MPF, MAP/ERK, MDM2/p53, NF-κB/IκB7 and PKA. Leptomycin B inhibits export of many RNAs, e.g. COX-2 and c-FOS mRNA. Leptomycin B also shows antifungal and antibacterial and potent antitumour activities.
Definition
ChEBI: A leptomycin having a (2E,10E,12E,16Z,18E)-double bond configuration as well as an ethyl substituent at position 17.
Biological Functions
Leptomycin B (LMB) is an unsaturated, branched-chain fatty acid that proved a potent tool in nuclear export studies. It was isolated from Streptomyces sp. strain ATS 1287. Until recently, LMB has been the only known small-molecule inhibitor of nuclear transport. The nuclear export inhibitor leptomycin B (LMB) prevents the export of proteins from the nucleus to the cytoplasm, protects p53 from Mdm2-mediated degradation, and potent inducer of p53 transcriptional activity. It is a specific inhibitor of the nuclear export of proteins containing leucine-rich nuclear export signal (NES). Supplementing sub-nanomolar concentrations of LMB to cultured cells caused inhibition of nuclear export of leucine-rich NES-bearing protein. Since its discovery as a potent inhibitor of nuclear export, a large number of shuttling proteins, performing a diverse range of cellular functions, are now known to accumulate in the nucleus.
General Description
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, I?B, MPF, PKA and MEK.
Biological Activity
Antifungal antibiotic that is an inhibitor of the nuclear export of proteins; acts by binding directly to and inhibiting CRM1/exportin-1. Inhibits the nuclear export of the HIV regulatory protein Rev and stabilizes p53. Antitumor in vitro and in vivo .
Mechanism of action
The nuclear export inhibition mechanism involves the direct binding of Leptomycin B to exportin1, which blocks the binding of exportin1 to proteins containing the leucine-rich NES. Later, NES-exportin1 interaction was identified on a conserved region near cysteine-529 residue of human exportin1. This cysteine-529 residue on exportin1 provides LMB sensitivity because unsaturated γ-lactone in LMB undergoes a Michael-type reaction by the sulfhydryl group on cysteine residue. Once LMB is bound to exportin1, the NES-bearing nuclear export cargo fails to bind the receptor.
Leptomycin B Preparation Products And Raw materials
Leptomycin B Suppliers
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Shanghai Minbiotech Co., Ltd. | +8617315815539 | CHINA | 129 | 58 | Inquiry |
| Fuxin Pharmaceutical | +86-021-021-50872116 +8613122107989 | China | 10297 | 58 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29826 | 58 | Inquiry |
| Shaanxi Dideu Medichem Co. Ltd | +86-029-81138252 +86-18789408387 | China | 2381 | 58 | Inquiry |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | China | 5738 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
| Hubei Ipure Biology Co., Ltd | +8613367258412 | China | 10326 | 58 | Inquiry |
| Shaanxi Dideu Medichem Co. Ltd | +86-029-89586680 +86-18192503167 | China | 9030 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 26165 | 58 | Inquiry |
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