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Purity: ≥98%
SQ22536 (formerly NSC-53339) is a novel and effective inhibitor of adenylyl cyclase (AC) with an IC50 of 1.4 μM. It can prevent intact human platelets from experiencing PGE1-stimulated increases in cAMP levels. SQ22536 (SQ22,536), with IC50 values of 5 μM, effectively inhibits the effect of forskolin. Gradient concentrations of SQ22536 preincubated with PACAP-induced reporter gene activation show that both SQ22536 effectively inhibits the process, with an approximate IC50 value of 5 μM. SQ22536 inhibits Elk activation induced by forskolin more potently than Elk activation induced by 8-Br-cAMP (IC50 = 170 μM; IC50 = 10 μM).
| Targets |
adenylate cyclase (AC)
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| Enzyme Assay |
SQ22536 inhibits Elk activation induced by forskolin more potently than Elk activation induced by 8-Br-cAMP (IC50 = 170 μM; IC50 = 10 μM).
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| Cell Assay |
Rat PAC1hop receptors are expressed by retroviral vectors that transduce HEK293 CRE-luc2P GloResponse luciferase reporter cells. By using limiting dilution cloning, individual cell lines are obtained. A clonal PAC1-expressing line is then propagated and employed in CRE luciferase assays. To summarize, assay media (DMEM supplemented with 1% fetal bovine serum) is used to plate HEK293 CRE-luc2P cells in 96-well plates (10,000 cells in 80 μL media per well). 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. Once 100 μL/well of Bright-Glo Luciferase Assay Reagent has been added, luciferase activity is measured. Luminescence (RLU) is measured in a Victor3 microtiter plate reader after 2 minutes of agitation at room temperature. Utilizing NS-1 cells, cyclic AMP is quantified. NS-1 cells are, in essence, seeded and grown in 96-well plates for an entire night. Cells are pretreated in media containing 3-isobutyl-1-methylxanthine (0.5 mM) phosphodiesterase inhibitor with or without SQ22536 for 20 minutes the following day. Agonists are added as 10× solutions and let to stimulate cells for 20 minutes after the cells have been pretreated with inhibitors. The quantification of nonacetylated cAMP is then achieved by measuring intracellular cAMP using the cAMP Biotrak enzyme immunoassay technique.
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| References |
| Molecular Formula |
C9H11N5O
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| Molecular Weight |
205.22
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| Exact Mass |
205.1
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| Elemental Analysis |
C, 52.67; H, 5.40; N, 34.13; O, 7.80
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| CAS # |
17318-31-9
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CC(OC1)N2C=NC3=C(N=CN=C32)N
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| InChi Key |
UKHMZCMKHPHFOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H11N5O/c10-8-7-9(12-4-11-8)14(5-13-7)6-2-1-3-15-6/h4-6H,1-3H2,(H2,10,11,12)
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| Chemical Name |
9-(oxolan-2-yl)purin-6-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (12.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (121.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8728 mL | 24.3641 mL | 48.7282 mL | |
| 5 mM | 0.9746 mL | 4.8728 mL | 9.7456 mL | |
| 10 mM | 0.4873 mL | 2.4364 mL | 4.8728 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Evaluation of cell-permeable AC inhibitors.Mol Pharmacol.2013 Jan;83(1):95-105. |
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SQ22,536 inhibits cAMP-dependent ERK phosphorylation, but not NGF or PMA-induced ERK phosphorylation.Mol Pharmacol.2013 Jan;83(1):95-105. |
SQ22,536 inhibits cAMP-dependent Elk activation.Mol Pharmacol.2013 Jan;83(1):95-105. |
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