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SKF-96365 hydrochloride

Catalog No. T2170   CAS 130495-35-1
Synonyms: SKF96365

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ/AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

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SKF-96365 hydrochloride Chemical Structure
SKF-96365 hydrochloride, CAS 130495-35-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 52.00
10 mg In stock $ 78.00
25 mg In stock $ 141.00
50 mg In stock $ 255.00
100 mg In stock $ 495.00
200 mg In stock $ 755.00
500 mg In stock $ 1,170.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 99.85%
Purity: 99.76%
Purity: 99.48%
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Biological Description
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Storage & Solubility Information
Description SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ/AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.
In vitro SKF-96365 exhibits protective activity against MPP+ injury in PC12 cells and significantly inhibits apoptotic cell death in PC12 cells after MPP+ administration. SKF-96365 does not exert effects on necrotic cell death induced by MPP+ insult in PC12 cells. Because of its non-selective activity, SKF-96365 has been demonstrated to have effects on multiple other Ca2+ channels: it not only blocks high-voltage-activated (HVA) Ca2+ channels at typically utilized test concentrations, but also potently inhibits low-voltage -activated (LVA) T-type Ca2+ channels in HEK293 cells. The exact effect of SKF-96365 on intracellular calcium homeostasis might dependent on cell types and experimental models used[2].
In vivo SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo[4].
Cell Research To investigate whether SKF-96365 could protect PC12 cells from injury induced by MPP+ insult, cultured PC12 cells are pretreated with SKF-96365 in different concentrations (1 µM, 10 µM or 50 µM) 30 min before MPP+ addition. The cells viability is measured 24 h after MPP+ insult by using the cell proliferation reagent WST-1. (Only for Reference)
Synonyms SKF96365
Molecular Weight 402.91
Formula C22H27ClN2O3
CAS No. 130495-35-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 198.6 mM

H2O: 198.6 mM

TargetMolReferences and Literature

1. Singh A, et al. Br J Pharmacol. 2010, 160(6):1464-1475. 2. Chen T, et al. PLoS One. 2013, 8(1):e55601. 3. Yao H, et al. Cell Death Differ. 2009, 16(12):1681-1693. 4. Jing Z, et al. Cancer Lett. 2016, 372(2):226-38.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Colorectal Cancer Compound Library NO PAINS Compound Library CNS-Penetrant Compound Library Anti-Cardiovascular Disease Compound Library Anti-COVID-19 Compound Library Metabolism Compound Library Anti-Hypertension Compound Library Anti-Aging Compound Library Inhibitor Library

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Keywords

SKF-96365 hydrochloride 130495-35-1 Apoptosis Autophagy Membrane transporter/Ion channel Metabolism Potassium Channel Calcium Channel TRP/TRPV Channel CRAC Channel Inhibitor SKF96365 Hydrochloride QTc anti-neoplastic arrest Ca2+ release-activated Ca2+ channels KcsA SKF 96365 SKF-96365 Hydrochloride prolong inhibit cell-cycle interval SKF-96365 Transient receptor potential channels SKF 96365 Hydrochloride colorectal SKF96365 cancer SKF96365 hydrochloride TRP Channel SKF 96365 hydrochloride Calcium release-activated channels inhibitor

 

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