SQ 22536

An adenylyl cyclase inhibitor

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10mg

￥762.00

610.00

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50mg

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Background

SQ22536 is an effective adenylate cyclase (AC) inhibitor.
SQ22536 (SQ22,536) effectively inhibits the effect of forskolin with respective IC50 values of 5 μM.Preincubation with graded concentrations of SQ22536 reveals that both SQ22536 effectively inhibits PACAP-induced reporter gene activation with approximate IC50 value of 5 μM. SQ22536 more potently inhibits forskolin-induced Elk activation (IC50=10 μM) than 8-Br-cAMP-induced Elk activation (IC50=170 μM). Most notably, there are substantial differences in the reported potencies of SQ22536 to inhibit the activities of recombinant AC5 and AC6, with respective IC50 values of 2 μM and 360 μM. At a greater concentration (500 μM), SQ22536 significantly inhibits neurite elongation due to either forskolin or 8-Br-cAMP[1].
Reference:
[1]. Emery AC, et al. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536. Mol Pharmacol. 2013 Jan;83(1):95-105.

Protocol

Cell experiment:

HEK293 CRE-luc2P GloResponse luciferase reporter cells are transduced with retroviral vectors expressing rat PAC1hop receptors. Individual cell lines are obtained by limiting dilution cloning, and a clonal PAC1-expressing line is propagated and used for CRE luciferase assays. In brief, HEK293 CRE-luc2P cells are plated in 96-well plates (10,000 cells in 80 μL media per well) in assay media (DMEM supplemented with 1% fetal bovine serum). One day after plating, cells are treated with AC inhibitors (10 μL in assay media/well) for 30 minutes, followed by agonists (10 μL in assay media/well), and are incubated for 4 hours. Luciferase activity is determined after the addition of 100 μL/well Bright-Glo Luciferase Assay Reagent. Luminescence (RLU) is measured in a Victor3 microtiter plate reader after 2 minutes of agitation at room temperature. Cyclic AMP is measured in NS-1 cells. In brief, NS-1 cells are seeded and grown overnight in 96-well plates. The next day, cells are pretreated for 20 minutes in media containing the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (0.5 mM) with or without SQ22536. After pretreatment with inhibitors, cells are stimulated with agonists, added as 10× solutions, for an additional 20 minutes. Intracellular cAMP is then assayed using the cAMP Biotrak enzyme immunoassay kit for measurement of nonacetylated cAMP[1].

参考文献:

[1]. Emery AC, et al. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536. Mol Pharmacol. 2013 Jan;83(1):95-105.