Drug intelligence / Profile preview

SKF96365

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Experimental (intraperitoneal In Animal Studies), In Vitro
01

Overview

SKF96365 is a **synthetic small molecule inhibitor** primarily recognized as a blocker of **receptor-operated and store-operated calcium entry (SOCE)** pathways by inhibiting **transient receptor potential canonical (TRPC) channels** and is also a **potent blocker of low-voltage-activated T-type calcium channels**. It has additionally demonstrated inhibitory activity against other channels, such as high-voltage-activated L-type calcium channels, some potassium channels, and others at higher concentrations[1][3][4][6]. It is frequently used in research on calcium signaling, cellular physiology, and oncology models. **SmithKline Beecham** originally developed SKF96365 for angina pectoris, but clinical development was terminated and it is now used exclusively as a research tool[1][3][4]. Preclinical studies have shown anti-proliferative and pro-apoptotic effects across multiple cancer cell types, largely through disruption of CaMKIIγ/AKT signaling and modulation of cell cycle and autophagy[3][6]. SKF96365 is not approved for clinical use and is for laboratory research only[1][2].

Other names
1-[2-(4-methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl]-1H-imidazole1-[2-(4-Methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl]imidazole1-[beta-[3-(4-Methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole1-(2-(3-(4-Methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1H-imidazole1-{2-(4-Methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl}-1H-imidazole hydrochlorideSKF-96365 free baseSKF96365 free baseSKF 96365 free base
02

Targets

CACNA1G (T-type Calcium Channel Protein Subunit Alpha-1G)CACNA1A (P-type Calcium Channel)CaV3 (Caveolin-3)SOCE (Calcium release-activated calcium channel)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)TRPC (TRPC family)CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)

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