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MAM03055A

Chemical Structure : MAM03055A

CAS No.: 3032973-86-4

MAM03055A (MAM 03055A)

Catalog No.: PC-47095Not For Human Use, Lab Use Only.

MAM03055A is a novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity, exhibits high affinity and strong preference for sigma-2 receptor with Ki of 55.9 nM.

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    Biological Activity

    MAM03055A is a novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity, exhibits high affinity and strong preference for sigma-2 receptor with Ki of 55.9 nM.
    MAM03055A displays weak affinity against sigma-1 receptor with Ki of 3371 nM.
    MAM03055A potently induced cell death in SK-N-SH neuroblastoma, MDA-MB-231 breast, and both SW48 and SW480 colorectal cancer cell lines, causing proapoptotic BH3 interacting-domain death agonist (BID) cleavage in SK-N-SH cells.
    MAM03055A bound pseudo-irreversibly to sigma-2 receptors and caused residual cytotoxic activity after acute exposure and removal of the compound from the media.
    MAM03055A also induced a time-dependent loss of sigma-2 receptor/TMEM97 protein from cells.

    Physicochemical Properties

    M.Wt 810.966
    Formula C43H48F2N8O4S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1,3-bis(3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)thiourea

    References

    1. Liu CZ, et al. Eur J Pharmacol. 2021 Sep 5;906:174263.

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