Name: 21-Hydroxyoligomycin A
Price: 416.00 USD

- Overview
  - 21-Hydroxyoligomycin A is a rare member of the Oligomycin class, isolated as a co-metabolite of nemadectin, hence it was originally named Nemadectin omega. Only limited literature references are available. In-house testing suggests that 21-Hydroxyoligomycin has a more selective action against mammalian tumor cell lines than Oligomycin A, exhibiting only weak antifungal and nematocidal activity. 21-Hydroxyoligomycin A can Inhibit K-Ras plasma membrane localization and is therefore a putative anti-cancer agent.
    21-Hydroxyoligomycin A is soluble in ethanol, methanol, DMF and DMSO but practically insoluble in water.
    
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    Background
    
    21-Hydroxyoligomycin A can inhibit K-Ras plasma membrane localization are therefore putative cancer chemotherapeutic agents. The study of its inhibitory mechanism of action are expected to reveal pathways and molecular targets to control K-Ras (Salim et al, 2016).
    Single-crystal X-ray analysis established the structure and absolute configuration of 21-Hydroxyoligomycin A (Wagenaar et al, 2017).
- Properties
  - CAS Number
    
    102042-09-1
    
    Molecular Formula
    
    C45H74O12
    
    Molecular Weight
    
    807.1
    
    Appearance
    
    White lyophilisate
    
    Solubility
    
    Soluble in ethanol, methanol, DMF and DMSO but practically insoluble in water.
    
    Other Properties
    
    Source: Streptomyces cyaneogriseus ssp. noncyanogenus (LL-F28249)
    Purity Level: >95% by HPLC
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    Cancer Applications: It is reported to be cytotoxic to human colon cancer SW620 cells (IC50 = 14.4 μM), and colorectal carcinoma cells (IC50 > 3 µM), to inhibit the ABC transporter efflux pump P-glycoprotein (P-gp). Ras proteins are membrane-bound GTPases that regulate cell growth, proliferation and differentiation. Mutant forms of Ras are prominent in many human cancers. Oncogenic mutant K-Ras must be localized to the plasma membrane to be functional. 21-Hydroxyoligomycin A prevented K-Ras plasma membrane localization (IC50 = 4.82 nM). Oligomycins A-E inhibited K-Ras plasma membrane localization with (IC50 range of ~ 1.5-14 nM (Wagenaar et al, 2007). Inhibitors of K-Ras plasma membrane localization are therefore putative cancer chemotherapeutic agents. The study of K-Ras inhibitory mechanism of action are expected to reveal pathways and molecular targets to control K-Ras. This could inform the development of new probes to better interrogate K-Ras-dependent cancers.

Datasheet

21-Hydroxyoligomycin A

21-Hydroxyoligomycin A

Background

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