1. SKF-96365 hydrochloride

SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells.

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SKF-96365 hydrochloride Chemical Structure

SKF-96365 hydrochloride Chemical Structure

CAS No. : 130495-35-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 72 In-stock
Solution
10 mM * 1 mL in DMSO USD 72 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 110 In-stock
50 mg USD 429 In-stock
100 mg USD 715 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 17 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • Customer Review

Description

SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells[1][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].

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

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].

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

Molecular Weight

402.91

Formula

C22H27ClN2O3

CAS No.
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: 

DMSO : 100 mg/mL (248.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (248.19 mM; Need ultrasonic)

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
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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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: 99.91%

Animal Administration
[2]

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].

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / 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.

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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.

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Product Name:
SKF-96365 hydrochloride
Cat. No.:
HY-100001
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