SKF-96365 hydrochloride

Name: SKF-96365 hydrochloride
Brand: MedChemExpress
SKU: HY-100001
Rating: 5.0 (27 reviews)

Cat. No.: HY-100001 Purity: 99.93%: Data Sheet
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SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia.

For research use only. We do not sell to patients.

CAS No. : 130495-35-1

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of SKF-96365 hydrochloride:

SKF-96365 In-stock

27 Publications Citing Use of MCE SKF-96365 hydrochloride

RT-PCR

Cell Migration/Invasion Assay

: SKF-96365 hydrochloride purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2025 Apr 24;16(1):206. [Abstract]; Western blot analysis of CaMKK2, AMPK activation and RUNX2 in MSCs after osteogenic differentiation for 72 h treated with TRP channel blocker SKF-96,365 hydrochloride (SKF, 2 µM) under control and nZnO (5 µg/mL) conditions.

: SKF-96365 hydrochloride purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Apr 21;6(11):4073-4082. [Abstract]; Intracellular calcium fluorescence staining of MC3T3-E1 cells on day 1 in a blank and samples inhibited by verapamil (10 μmol/L, 24 h) or SKF-96365 (10 μmol/L, 24 h).

: SKF-96365 hydrochloride purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Apr 21;6(11):4073-4082. [Abstract]; SKF-96365 (100 μM; 2 h) significantly inhibits the mRNA levels of the HSV-1 UL30 gene in Trpv2^fl/fl BMDCs but not in Lyz2-Cre;Trpv2^fl/fl BMDCs.

: SKF-96365 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]; WB were applied to measure levels of Nanog, Oct-4, Sox2 and ALB in FGF19 (100 ng/ml) treated NCSCs, in the presence of SKF-96365 (5 µM) or not.

: SKF-96365 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 May 16;10(14):6483-6499. [Abstract]; Transwell assays were performed to detect the effects of different concentrations SKF-96365 on the invasion ability of Snail1 OE-SMMC7721 and HepG2 cells. The results show that SKF-96365 (2-5 μM) enhances the invasive ability of hepatocellular carcinoma cells with Snail1 overexpression.

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TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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CaMK II CaMK III/eEF-2K CAMK IV PHK Trio DCAMKL

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Akt Akt1 Akt2 Akt3

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

SKF-96365 (0-10 μM; applied until steady-state inhibition is reached) hydrochloride inhibits hNaV1.5 currents stably expressed in HEK 293 cells, with an IC₅₀ of 0.94 μM^[2].
SKF-96365 (0-20 μM) hydrochloride dose-dependently inhibits store-operated calcium entry in human colorectal cancer cell lines HCT116 and HT29^[3].
SKF-96365 (0-40 μM, 48-72 h) hydrochloride inhibits the growth of human colorectal cancer cells HCT116 (IC₅₀ = 10.88 μM) and HT29 (IC₅₀ = 14.56 μM), and exhibits significantly lower toxicity against normal colonic epithelial cells NCM460^[3].
SKF-96365 (0-20 μM, 48 h) hydrochloride induces G₂/M cell cycle arrest in human colorectal cancer cells HCT116 and HT29 by regulating key G₂/M transition proteins, including upregulating p21waf/Cip1 and downregulating p-Cdc25c, Cdc25c, and Cyclin B^[3].
SKF-96365 (10 μM, 0-24 h) hydrochloride induces apoptosis in human colorectal cancer cell lines HCT116 and HT29 via the endogenous mitochondrial pathway, a process characterized by early (12 h) mitochondrial membrane depolarization, Bax translocation and cytochrome c release, followed by caspase activation and marked apoptosis (24 h)^[3].
SKF-96365 (0-20 μM, 12 h) hydrochloride induces cytoprotective autophagy in human colorectal cancer cells HCT116 and HT29. This effect appears as early as 12 h (prior to apoptosis) and antagonizes apoptosis by sequestering mitochondria into autophagosomes to reduce cytosolic cytochrome c levels^[3].
SKF-96365 (0-20 μM, 24 h) hydrochloride inhibits the AKT/mTOR signaling pathway and the calcium/Ca²⁺/CaMKIIγ/AKT signaling pathway in human colorectal cancer cell lines HCT116 and HT29^[3].
SKF-96365 (1-50 μM, 24 h) hydrochloride significantly increases the survival rate of PC12 cells treated with MPP⁺, reduces LDH release, alleviates nuclear damage, membrane damage, and late apoptotic cell death, mitigates intracellular calcium overload, and decreases the mRNA and protein expression levels of Homer1^[4].
SKF-96365 (1-10 µM) hydrochloride inhibits melittin-induced inward currents in acutely isolated small and medium-sized dorsal root ganglion cells of rats in a dose-dependent manner^[5].
SKF-96365 (10 µM) hydrochloride inhibits melittin-induced intracellular Ca²⁺ elevation, and the proportion of cells exhibiting this inhibitory effect reaches 46.5% in acutely isolated rat dorsal root ganglion cells sensitive to melittin^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[4]

Cell Line:	PC12 (adrenal gland pheochromocytoma) cells
Concentration:	1 μM, 10 μM, 50 μM
Incubation Time:	30 min pretreatment before MPP+ insult; 24 h post-MPP+ measurement
Result:	Significantly inhibited the MPP⁺-induced decrease in cell viability at 10 μM and 50 μM, with viability levels significantly higher than the MPP+-treated vehicle group. Did not show a significant effect on cell viability compared to the vehicle group at 1 μM. Did not affect cell viability in untreated normal PC12 cells at all tested concentrations.

Apoptosis Analysis^[4]

Cell Line:	PC12 cells
Concentration:	50 μM
Incubation Time:	30 min pretreatment before MPP+ insult; 24 h post-MPP+ flow cytometry
Result:	Increased the percentage of normal (AV^-/PI^-) cells compared to the MPP+-treated vehicle group. Decreased the percentage of late apoptotic (AV⁺/PI⁺) cells compared to the MPP+-treated vehicle group. Showed no significant effect on necrotic (AV^-/PI⁺) cells.

Real Time qPCR^[4]

Cell Line:	PC12 cells
Concentration:	50 μM
Incubation Time:	30 min pretreatment before MPP+ insult; measured at 3 h, 6 h, 12 h post-MPP+
Result:	Significantly decreased Homer1 mRNA expression in a time-dependent manner, with significant reductions observed at 3 h, 6 h, and 12 h post-MPP+ insult compared to the MPP+-treated vehicle group. MPP+ alone did not alter Homer1 mRNA expression compared to untreated control cells.

Western Blot Analysis^[4]

Cell Line:	PC12 cells
Concentration:	50 μM
Incubation Time:	30 min pretreatment before MPP+ insult; 24 h post-MPP+ measurement
Result:	Significantly decreased Homer1 protein expression in a time-dependent manner, with significant reductions observed at 3 h, 6 h, and 12 h post-MPP+ insult compared to the MPP+-treated vehicle group. MPP+ alone did not alter Homer1 protein expression compared to untreated control cells.

In Vivo

SKF-96365 (200-400 μg; intranasal administration; once daily; for 8 consecutive days) hydrochloride dose-dependently alleviates allergic rhinitis symptoms and suppresses inflammatory responses in BALB/c mice^[1].
SKF-96365 (20 mg/kg; i.p.; once daily for 14 consecutive days) hydrochloride inhibits the growth of colorectal cancer xenografts in athymic BALB/c nude mice by inducing cell cycle arrest, apoptosis and protective autophagy via suppressing the CaMKIIγ/AKT-mediated pathway^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c (female; allergic rhinitis model via intraperitoneal sensitization and intranasal challenge)^[1]
Dosage:	200 μg; 400 μg
Administration:	i.n.; once daily; 8 days (1 hour before ovalbumin challenge)
Result:	Significantly reduced frequencies of sneezing and nasal rubbing compared to untreated allergic rhinitis mice, with the 400 μg dose being more effective than the 200 μg dose. Significantly decreased serum levels of OVA-specific IgE, histamine, and LTC4 compared to untreated allergic rhinitis mice, with greater reductions observed in the 400 μg group. Significantly decreased nasal lavage fluid levels of OVA-specific IgE, IL-4, IL-5, IL-6, IL-13, and IL-33 compared to untreated allergic rhinitis mice, with greater reductions observed in the 400 μg group. Significantly decreased counts of total inflammatory cells, eosinophils, macrophages, neutrophils, and lymphocytes in nasal lavage fluid compared to untreated allergic rhinitis mice, with greater reductions observed in the 400 μg group. Reduced eosinophil counts in nasal mucosa compared to untreated allergic rhinitis mice, with the 400 μg dose producing more pronounced effects than the 200 μg dose. Downregulated TRPC6 immunolabeling in nasal mucosa compared to untreated allergic rhinitis mice, with the 400 μg dose producing more pronounced effects than the 200 μg dose. Decreased nasal mucosa mRNA levels of TRPC6, STIM1, and Orai1 compared to untreated allergic rhinitis mice, with the 400 μg dose producing more pronounced effects than the 200 μg dose.

Molecular Weight

402.91

Formula

C₂₂H₂₇ClN₂O₃

CAS No.

130495-35-1

Appearance

Solid

Color

White to light yellow

SMILES

COC1=CC=C(CCCOC(C2=CC=C(OC)C=C2)CN3C=CN=C3)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (248.19 mM; Need ultrasonic; DMSO can inactivate SKF-96365 hydrochloride's activity)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4819 mL	12.4097 mL	24.8194 mL
5 mM	0.4964 mL	2.4819 mL	4.9639 mL
10 mM	0.2482 mL	1.2410 mL	2.4819 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Saline
Solubility: 100 mg/mL (248.19 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (286 KB) SDS (394 KB)

COA (248 KB) HNMR (262 KB) RP-HPLC (249 KB) LCMS (325 KB)

Handling Instructions (2659 KB)

References

[1]. Ba G, et al. Therapeutic effects of SKF-96365 on murine allergic rhinitis induced by OVA. Int J Immunopathol Pharmacol. 2021;35:20587384211015054.

[2]. Chen KH, et al. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. Pflugers Arch. 2015;467(6):1227-1236.

[3]. 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;372(2):226-238. [Content Brief]

[4]. Chen T, et al. Protective effects of SKF-96365, a non-specific inhibitor of SOCE, against MPP+-induced cytotoxicity in PC12 cells: potential role of Homer1. PLoS One. 2013;8(1):e55601. [Content Brief]

[5]. Ding J, et al. Effects of SKF-96365, a TRPC inhibitor, on melittin-induced inward current and intracellular Ca2+ rise in primary sensory cells. Neurosci Bull. 2011;27(3):135-142.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	2.4819 mL	12.4097 mL	24.8194 mL	62.0486 mL
	5 mM	0.4964 mL	2.4819 mL	4.9639 mL	12.4097 mL
	10 mM	0.2482 mL	1.2410 mL	2.4819 mL	6.2049 mL
	15 mM	0.1655 mL	0.8273 mL	1.6546 mL	4.1366 mL
	20 mM	0.1241 mL	0.6205 mL	1.2410 mL	3.1024 mL
	25 mM	0.0993 mL	0.4964 mL	0.9928 mL	2.4819 mL
	30 mM	0.0827 mL	0.4137 mL	0.8273 mL	2.0683 mL
	40 mM	0.0620 mL	0.3102 mL	0.6205 mL	1.5512 mL
	50 mM	0.0496 mL	0.2482 mL	0.4964 mL	1.2410 mL
	60 mM	0.0414 mL	0.2068 mL	0.4137 mL	1.0341 mL
	80 mM	0.0310 mL	0.1551 mL	0.3102 mL	0.7756 mL
	100 mM	0.0248 mL	0.1241 mL	0.2482 mL	0.6205 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.