SKU: H032  / 
    CAS Number: 102042-09-1

    21-Hydroxyoligomycin A

    ₹34,024.28 - ₹118,502.57
    • Detailed Description

      CAS Number: 102042-09-1

      Molecular Formula: C45H74O12

      Molecular Weight: 807.1

      Mechanism of Action: 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).

      Storage Conditions: -20°C

    • Applications

      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.

    • Specifications

      Appearance: White lyophilisate

      Source: Streptomyces cyaneogriseus ssp. noncyanogenus (LL-F28249)

      Purity Level: >95% by HPLC

    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. 

    We also offer:

    • Oligomycin (O037)
    • Oligomycin A (O013)
    • Oligomycin B (O018)
    • Oligomycin C (O019)
    • Oligomycin D (O020)
    • Oligomycin E (O021)
    • 21-Hydroxyoligomycin A (H032)

    CAS Number: 102042-09-1

    Molecular Formula: C45H74O12

    Molecular Weight: 807.1

    Mechanism of Action: 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).

    Storage Conditions: -20°C

    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.

    Appearance: White lyophilisate

    Source: Streptomyces cyaneogriseus ssp. noncyanogenus (LL-F28249)

    Purity Level: >95% by HPLC