SKF96365|SKF-96365|cas 130495-35-1

Cas No.:	130495-35-1
Chemical Name:	SKF-96365 HCl
Synonyms:	SKF-96365，SKF 96365
SMILES:	C1N(CC(OCCCC2=CC=C(OC)C=C2)C2=CC=C(OC)C=C2)C=CN=1.[H]Cl
Formula:	C₂₂H₂₇ClN₂O₃
M.Wt:	402.92
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
Target:	TRP Channel[1]
In Vivo:	SKF-96365 inhibits 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].
In Vitro:	SKF-96365 exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells. SKF-96365 inhibits hERG current in a concentration-dependent manner[1]. SKF-96365 can induces cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 treatment inhibits the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade. Overexpression of CaMKIIγ or AKT abolishes the effects of SKF-96365 on cancer cells, suggesting a critical role of the CaMKIIγ/AKT signaling pathway in SFK-96365-induced biological effects[2].
Animal Administration:	Mice: Five to six-week-old female athymic BALB/c mice are inoculated into the right oxter with HCT116 cells. When the diameter of the subcutaneous tumor reaches approximately 0.5 cm, animals are randomLy assigned to the vehicle, SKF-96365 alone, HCQ alone or SKF-96365+HCQ. SKF-96365 is applied (20 mg/kg) and HCQ is applied (60 mg/kg) daily for 14 successive days by i.p. injection. Tumor sizes and volume are determined. Eight mice are included in each group. Mice are sacrificed 24 h after the last treatment. The tumors are weighed and processed for western blot analysis or paraffin embedding[2].
References:	[1]. Liu H, et al. SKF-96365 blocks human ether-à-go-go-related gene potassium channels stably expressed in HEK 293 cells. Pharmacological 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 the calcium/CaMKIIγ/AKT-mediated pathway. Cancer Lett, 2016 Mar 28, 372(2):226-38.

Cat. No.	Product name	Field of application
DC72365	BAY-390	BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively.
DC70461	GSK3527497	GSK3527497 (GSK-3527497) is a potent, selective TRPV4 inhibitor with IC50 of 12 nM (hTRPV4).GSK3527497 is a pre-clinical candidate for treatment of diseases resulting from TRPV4 activation.
DC70460	GSK3395879	GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4); exhibits little or no activity against a broad panel of TRP channels (IC50 > 10µM for TRPA1, TRPV1, TRPM2, TRPM4, TRPM8, TRPC3, TRPC4, TRPC5, TRPC6); demonstrates the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model.
DC11472	TRPM8 antagonist 14	TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
DC7755	TRCP6 inhibitor(SAR7334)	TRPC6 inhibitor is a potent TRPC6(Transient receptor potential cation channel, subfamily C, member 6) inhibitor.
DC9722	SKF96365	SKF96365 is blocker of TRP cation channels. Inhibits capacitative Ca2+ entry.
DC9635	SB-705498	SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
DC9735	SB-366791	SB-366791 is a selective and competitive VR1 (TRPV1) antagonist that is commonly used in pain research.
DC8306	RQ-00203078	RQ-00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively).
DC7262	Optovin	Optovin is a reversible photoactive TRPA1 activator.