2. Membrane Transporter/Ion Channel Neuronal Signaling PI3K/Akt/mTOR Apoptosis Autophagy
  3. CRAC Channel TRP Channel CaMK Akt Apoptosis Autophagy Na+/Ca2+ Exchanger Calcium Channel
  4. SKF-96365

SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 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. : 162849-90-3

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Based on 27 publication(s) in Google Scholar

Other Forms of SKF-96365:

SKF-96365 Related Antibodies

Top Publications Citing Use of Products

27 Publications Citing Use of MCE SKF-96365

IF
RT-PCR
Cell Migration/Invasion Assay
WB

    SKF-96365 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 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 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 Trpv2fl/fl BMDCs but not in Lyz2-Cre;Trpv2fl/fl BMDCs.

    SKF-96365 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 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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    N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

    • Biological Activity

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    Description

    SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia[1][2][3][4][5].

    In Vitro

    SKF-96365 (0-10 μM; applied until steady-state inhibition is reached) inhibits hNaV1.5 currents stably expressed in HEK 293 cells, with an IC50 of 0.94 μM[2].
    SKF-96365 (0-20 μM) 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) 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) 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) 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) 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) 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) 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) 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) 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.

    SKF-96365 Related Antibodies

    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; measured at 3 h, 6 h, 12 h post-MPP+
    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) 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) 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: athymic BALB/c nude (5-6-week-old female; subcutaneous xenograft model via HCT116 cell inoculation)[3]
    Dosage: 20 mg/kg
    Administration: i.p.; daily; 14 days
    Result: Reduced tumor growth compared to vehicle control.
    Decreased tumor tissue expression of phosphorylated AKT (p-AKT) and proliferating cell nuclear antigen (PCNA).
    Increased expression of cleaved caspase-3 and LC3-II.
    Decreased levels of phosphorylated CaMKII (p-CaMKII) and p-AKT in tumor lysates via western blot analysis.
    Increased levels of LC3-II, cleaved PARP, cleaved caspase-3, and cleaved caspase-9 in tumor lysates via western blot analysis.
    Caused no significant weight loss or liver/kidney injury.
    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

    366.45

    Formula

    C22H26N2O3
    CAS No.
    Appearance

    Oil

    Color

    Colorless to light yellow

    SMILES

    COC1=CC=C(CCCOC(C2=CC=C(OC)C=C2)CN3C=CN=C3)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (272.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7289 mL 13.6444 mL 27.2889 mL
    5 mM 0.5458 mL 2.7289 mL 5.4578 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo:

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    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (13.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 5 mg/mL (13.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
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    Purity & Documentation
    References

    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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7289 mL 13.6444 mL 27.2889 mL 68.2221 mL
    5 mM 0.5458 mL 2.7289 mL 5.4578 mL 13.6444 mL
    10 mM 0.2729 mL 1.3644 mL 2.7289 mL 6.8222 mL
    15 mM 0.1819 mL 0.9096 mL 1.8193 mL 4.5481 mL
    20 mM 0.1364 mL 0.6822 mL 1.3644 mL 3.4111 mL
    25 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7289 mL
    30 mM 0.0910 mL 0.4548 mL 0.9096 mL 2.2741 mL
    40 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7056 mL
    50 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3644 mL
    60 mM 0.0455 mL 0.2274 mL 0.4548 mL 1.1370 mL
    80 mM 0.0341 mL 0.1706 mL 0.3411 mL 0.8528 mL
    100 mM 0.0273 mL 0.1364 mL 0.2729 mL 0.6822 mL
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    SKF-96365 Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SKF-96365162849-90-3SKF96365SKF 96365CRAC ChannelTRP ChannelCaMKAktApoptosisAutophagyNa+/Ca2+ ExchangerCalcium ChannelCalcium release-activated channelsCa2+ release-activated Ca2+ channelsTransient receptor potential channelsCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesPKBProtein kinase BCa2+ channelsCa channelsstore-operated calcium entryOrai1TRPC channelAKT signalingPC12 cellscolorectal cancer cellsdorsal root ganglion cellsTRPC6CaMKIIγSTIM1Inhibitorinhibitorinhibit

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