NS8593
Based on 1 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.
Publications Citing Use of MedChemExpress (MCE) NS8593
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
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.
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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 (1)
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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
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)