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Chemical Structure : Calmirasone1
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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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.
| M.Wt | 401.429 | |
| Formula | C23H22F3NO2 | |
| Appearance | Solid | |
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1. Sunday Okutachi, et al. Front Cell Dev Biol. 2021 Jul 8;9:665673.
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