SKA-31

Alias: SKA31 SKA 31 SKA-31
Cat No.:V14863 Purity: ≥98%
SKA-31 is a potassium channel activator.
SKA-31 Chemical Structure CAS No.: 40172-65-4
Product category: Potassium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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50mg
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Product Description
SKA-31 is a potassium channel activator. The EC50s for KCa3.1, KCa2.2, KCa2.1 and KCa2.3 are 260 nM, 1.9 μM, 2.9 μM and 2.9 μM respectively. It can enhance Endothelial-derived hyperpolarizing factor response, lowering blood pressure.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
More specifically than other ion channels, SKA-31 inhibits KCa2/3 channels and activates them more effectively than PK 26124 [1]. In HCT-116 cells and HCT-8 cells, the IC50 values for SKA-31 are 5.3 μM and 46.9 μM, respectively [2]. SKA-31 (5.3 μM; 0-96 hours) decreases the swelling of HCT-116 cells [2]. HCT-116 cells are activated by SKA-31 (5 μM), and SKA-31 at 45 μM raises the proportion of G0/G1 phase cells in HCT-116 and HCT-8 cell lines at concentrations of 5 μM and 45 μM, respectively[2]. SKA-31 decreases CDDP-induced Akt phosphorylation and increases Caspase 3 activation [2]. Additionally effective at preventing HCT-116 cell proliferation are SKA-31 and CDDP [2].
ln Vivo
SKA-31 exhibits favorable pharmacokinetic characteristics and no acute effects [1]. SKA-31 activates KCa3.1 and KCa2.3 in vascular endothelial cells and increases myocardial choline Induced endothelium-derived epidermal hyperplatelet (EDHF)-mediated vasodilation [1]. It also enhances native KCa3.1 and KCa2.3 in carotid endothelial cells. 1.6 μM and 225 nM, in that order[1]. SKA-31 (1-30 mg/kg; ip) decreases glycemic MAP in normal wild-type mice during a 24-day period, but not KCa3.1. It also improves EDHF-type vasodilation and lowers glycemia in mice.
Cell Assay
Cell viability assay [2]
Cell Types: HCT-116 cells, HCT-8 cells
Tested Concentrations:
Incubation Duration: 24 hrs (hours)
Experimental Results: Cell viability was diminished in HCT-116 and HCT-8, with IC50s of 5.3 μM and 46.9 μM respectively.

Cell proliferation assay[2]
Cell Types: HCT-116 Cell
Tested Concentrations: 5.3 μM
Incubation Duration: 0-96 hrs (hours)
Experimental Results: HCT-116 cell proliferation diminished when IC50S value was added at time zero.

Apoptosis analysis [2]
Cell Types: HCT-116 cells, HCT-8 cells
Tested Concentrations: 5 μM (HCT-116 cells), 45 μM (HCT-8 cells)
Incubation Duration: 24 hrs (hours)
Experimental Results: Triggered HCT-116 cells apoptosis, and the effect was smaller in HCT-8 cells.

Cell cycle analysis[2]
Cell Types: HCT-116 cells, HCT-8 Cell
Tested Concentrations: 5 μM (HCT-116), 45 μM (HCT-8)
Incubation Duration: 24 hrs (hours)
Experimental Results: G0/% increase in cells HCT-116 and G1 phase of HCT-8 cell line.

Western Blot Analysis [2]
Cell Types: HCT-116 cells
Tested Concentrations:
Incubation Duration: 24 hrs (hours)
Experimental Results: When HCT-116 cells were co-treated with CDDP, Caspase 3 was fur
Animal Protocol
Animal/Disease Models: 16-25 weeks of mice[1]
Doses: 1 mg/kg, 10 mg/kg, 30 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: -/-) Mouse (-/-) MAP[1] . Normotensive wild-type mice had lower MAP over 24 hrs (hrs (hours)), but not KCa3.1(-/-) mice(-/-).
References
[1]. Sankaranarayanan A, et al. Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure. Mol Pharmacol. 2009 Feb;75(2):281-95.
[2]. Serena Pillozzi, et al. The combined activation of KCa3.1 and inhibition of Kv11.1/hERG1 currents contribute to overcome CDDP resistance in colorectal cancer cells. Br J Cancer. 2018 Jan; 118(2): 200–212.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H8N2S
Molecular Weight
200.259
Exact Mass
200.04
CAS #
40172-65-4
SMILES
S1C(N([H])[H])=NC2=C1C([H])=C([H])C1=C([H])C([H])=C([H])C([H])=C21
Synonyms
SKA31 SKA 31 SKA-31
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~624.19 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.9935 mL 24.9675 mL 49.9351 mL
5 mM 0.9987 mL 4.9935 mL 9.9870 mL
10 mM 0.4994 mL 2.4968 mL 4.9935 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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