SKF-96365-hydrochloride - TRP Channel 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESKF-96365 hydrochlorideCat. No.: HY-100001CAS No.: 130495-35-1分式: CHClNO分量: 402.91作靶點(diǎn): TRP Channel; Autophagy作通路: Membrane Transporter/Ion Channel; Neuronal Signaling;Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (248.19 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4819 mL 12.4097 mL 24.8194 mL5 mM 0.4964 mL 2.4819 mL 4.9639 mL10 mM 0.2482 mL 1.2410 mL 2.4819 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰?/p>

3、制澄清的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.20 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.20 mM); Clear solution3. 請依序

4、添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.20 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 SKF-96365 hydrochloride選擇性的TRP通道抑制劑。IC50 & Target TRP Channel 1體外研究 SKF-96365 exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and

5、 apoptosis in colorectalcancer cells. SKF-96365 inhibits hERG current in a concentration-dependent manner 1. SKF-96365 caninduces cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) fromthe mitochondria into the cytoplasm. Mechanistically, SKF-96365 treatmen

6、t inhibits the calcium/calmodulin-dependent protein kinase II (CaMKII)/AKT signaling cascade. Overexpression of CaMKII or AKTabolishes the effects of SKF-96365 on cancer cells, suggesting a critical role of the CaMKII/AKT signalingpathway in SFK-96365-induced biological effects 2.體內(nèi)研究 SKF-96365 inhi

7、bits CRC cell growth in vivo. SKF-96365 treatment results in a decrease of p-CaMKII and p-AKT as well as an increase in LC3-II, cleaved PARP, caspase-3, and caspase-9 in mice 2.PROTOCOLAnimal Mice: Five to six-week-old female athymic BALB/c mice are inoculated into the right oxter with HCT116 cells.

8、Administration 2 When the diameter of the subcutaneous tumor reaches approximately 0.5 cm, animals are randomLyassigned to the vehicle, SKF-96365 alone, HCQ alone or SKF-96365+HCQ. SKF-96365 is applied (20mg/kg) and HCQ is applied (60 mg/kg) daily for 14 successive days by i.p. injection. Tumor size

9、s and volumeare determined. Eight mice are included in each group. Mice are sacrificed 24 h after the last treatment. Thetumors are weighed and processed for western blot analysis or paraffin embedding 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶

10、使本產(chǎn)品發(fā)表的科研獻(xiàn) FASEB J. 2019 Jun 5:fj201802550R. Acta Biochim Biophys Sin (Shanghai). 2019 Aug 5;51(8):767-777.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Liu H, et al. SKF-96365 blocks human ether-go-go-related gene potassium channels stably expressed in HEK 293 cells.Pharmaco

11、logical Research. Pharmacol Res, 2016 Feb, 104:61-9.2. Jing Z, et al. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of thecalcium/CaMKII/AKT-mediated pathway. Cancer Lett, 2016 Mar 28, 372(2):226-38.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not