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Calmirasone1

Chemical Structure : Calmirasone1

CAS No.:

Calmirasone1 (Calmirasone 1)

Catalog No.: PC-72352Not For Human Use, Lab Use Only.

Calmirasone1 (Calmirasone 1) is a novel and potent covalent calmodulin (CaM) inhibitor with Kd of 0.87 uM.

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    Biological Activity

    Calmirasone1 (Calmirasone 1) is a novel and potent covalent calmodulin (CaM) inhibitor with Kd of 0.87 uM.
    Calmirasone1 shows potency in 3D spheroids with IC50 value of 12 uM (MDA-MB-231) and 5.2 uM (Hs 578T).
    Calmirasone1 has a 4-fold increased affinity for CaM as compared to OphA (Ophiobolin A) and was active against K-Ras in cells within minutes, as compared to hours required by OphA.
    Calmirasone1 displayed a 2.5-4.5-fold higher selectivity for KRAS over BRAF mutant 3D spheroid growth than OphA.
    Calmirasone1 has a 40-260-fold lower unspecific toxic effect on HRAS mutant cells, while it reaches almost 50% of the activity of novel K-RasG12C specific inhibitors in 3D spheroid assays.

    Physicochemical Properties

    M.Wt 401.429
    Formula C23H22F3NO2
    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

    8-isopropyl-3-oxo-2-(piperidin-1-yl)-4-(trifluoromethyl)-3H-benzo[cd]azulene-1-carbaldehyde

    References

    1. Sunday Okutachi, et al. Front Cell Dev Biol. 2021 Jul 8;9:665673.

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