NS8593 

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 (K_d = 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^[1][2].

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 (K_d = 0.47 μM at 0.3 μM Ca²⁺ and K_d = 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.

263.34

C₁₇H₁₇N₃

875755-39-8

C1(N[C@@H]2CCCC3=C2C=CC=C3)=NC4=CC=CC=C4N1

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• [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.