NS8593
Based on 2 publication(s) in Google Scholar
NS8593 is an SK channel (small conductance Ca2+-activated K+ channels) inhibitor. NS8593 reversibly inhibited recombinant SK3-mediated currents (human SK3 and rat SK3). NS8593 inhibits all the SK1-3 subtypes Ca2+-dependently (Kd = 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+). NS8593 does not affect the Ca2+-activated K channels of intermediate and large conductance (hlk and hBK channels, respectively). NS8593 can also inhibit TRPM7 (melastatin-related TRP cation channel 7) (IC50 = 1.6 mM). NS8593 can be used for the study of central nervous system (CNS) related diseases.
For research use only. We do not sell to patients.
- CAS No.: 875755-39-8
- Formula: C17H17N3
- Molecular Weight:263.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) NS8593
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
0.4 μM
Compound: 14, NS-8593
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Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique
Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique
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[PMID: 18998663] |
| HEK293 | EC50 |
0.44 μM
Compound: 14, NS-8593
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Inhibition of human SK3 channel Q493A;D495A mutant expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique
Inhibition of human SK3 channel Q493A;D495A mutant expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique
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[PMID: 18998663] |
| HEK293 | EC50 |
2.2 μM
Compound: 14, NS-8593
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Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique in presence of 500 nM Ca2+
Inhibition of wild type human SK3 channel expressed in HEK293 cells assessed as Ca2+ sensitivity by inside-out patch clamp technique in presence of 500 nM Ca2+
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[PMID: 18998663] |
In Vitro
NS8593 reversibly suppresses SK3 current; IC50 is 91 nM in HEK293 cells[1].
NS8593 (10 μM, 4 min) has no significant effect on human IK (hIK) current in HEK293 cells[1].
NS8593's (3 μM) inhibitory effect on HEK293 cells decreased with increasing intracellular Ca2+ concentration (Kd = 0.47 μM at 0.3 μM Ca2+ and Kd = 14 μM at 10 μM Ca2+)[1].
NS8593 (3 μM, 4 min) shifts the Ca2+ activation curve to the right (EC50 increases from 0.43 μM to 1.6 μM) and reduces the Hill coefficient (from 5.6 to 2.0) in HEK293 cells[1].
NS8593 cannot displace the binding of lapamin at a concentration of 10 μM, while lapamin, UCL 1684 and dequalinium completely inhibit the binding in HEK293 cells[1].
NS8593 (1 μM, 30 μM) reversibly suppresses TRPM7 current in HEK 293 cells; 1 μM NS8593 partially suppresses it, and 30 μM almost completely suppresses it; in solution without Mg2+, the IC50 is 1.6 μM; in the presence of 300 μM Mg2+, the IC50 increases to 5.9 μM[2].
NS8593 (10-100 μM) inhibits TRPM3 current in HEK293 cells (IC50 = 26.7 μM), but is specific for TRPM7 at 10 μM and does not affect TRPM8, TRPM2, TRPM5, TRPC6, TRPV1 or TRPA1[2].
NS8593 (10-30 μM, 24-48 h), following long-term exposure, inhibits TRPM7-dependent changes in HEK293 cell motility and morphology, confirming the role of TRPM7 in cell migration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Tetracycline-inducible HEK 293 cells expressing human TRPM7
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Concentration:10 μM, 30 μM
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Incubation Time:24 h
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Result:Significantly reduced the area of wound closure.
Chemical Information
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CAS No. 875755-39-8
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Molecular Weight 263.34
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Formula C17H17N3
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SMILES
C1(N[C@@H]2CCCC3=C2C=CC=C3)=NC4=CC=CC=C4N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Osmotic Tension Asymmetry Drives Electrotactic Migration via PDLIM7-Polarized Microfilament Coordination in Breast Cancer Cells. [Abstract]2025 Dec 22:e15246. PMID: 41431193 -
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
[1]. 1. Strøbaek D, et al. Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons. Mol Pharmacol. 2006 Nov;70(5):1771-82. [Content Brief]
[2]. 2. Chubanov V, et al. Natural and synthetic modulators of SK (K(ca)2) potassium channels inhibit magnesium-dependent activity of the kinase-coupled cation channel TRPM7. Br J Pharmacol. 2012 Jun;166(4):1357-76. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NS8593 Related Classifications
HY-137952 Related Classifications
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