Calmirasone1 | Calmodulin inhibitor | Probechem Biochemicals

Chemical Structure : Calmirasone1

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Calmirasone1 (Calmirasone 1)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	401.429
分子式	C23H22F3NO2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

Calmirasone1 (Calmirasone 1)

生物&药学活性

物理化学性质&存储条件

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Calmirasone1 (Calmirasone 1)

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