HJC 0350EPAC2 antagonist, potent and selective CAS# 885434-70-8 |
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Quality Control & MSDS
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| Cas No. | 885434-70-8 | SDF | Download SDF |
| PubChem ID | 22200891 | Appearance | Powder |
| Formula | C15H19NO2S | M.Wt | 277.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 33.33 mg/mL (120.16 mM; Need ultrasonic) | ||
| Chemical Name | 2,4-dimethyl-1-(2,4,6-trimethylphenyl)sulfonylpyrrole | ||
| SMILES | CC1=CC(=C(C(=C1)C)S(=O)(=O)N2C=C(C=C2C)C)C | ||
| Standard InChIKey | AFZWZVLPIMHLSE-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H19NO2S/c1-10-6-12(3)15(13(4)7-10)19(17,18)16-9-11(2)8-14(16)5/h6-9H,1-5H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective Epac2 inhibitor (IC50 = 0.3 μM). Displays no effect on Epac1. Blocks stimulation of the Epac2-FL FRET sensor in HEK293 cells. |
HJC 0350 Dilution Calculator
HJC 0350 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.6052 mL | 18.0258 mL | 36.0516 mL | 72.1033 mL | 90.1291 mL |
| 5 mM | 0.721 mL | 3.6052 mL | 7.2103 mL | 14.4207 mL | 18.0258 mL |
| 10 mM | 0.3605 mL | 1.8026 mL | 3.6052 mL | 7.2103 mL | 9.0129 mL |
| 50 mM | 0.0721 mL | 0.3605 mL | 0.721 mL | 1.4421 mL | 1.8026 mL |
| 100 mM | 0.0361 mL | 0.1803 mL | 0.3605 mL | 0.721 mL | 0.9013 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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HJC 0350 is a potent and selective antagonist of EPAC2 with IC50 value of 0.3 μM [1].
cAMP/cAMP regulated guanine nucleotide exchange factor (EPAC/cAMP-GEF) is a guanine nucleotide exchange factor for the small GTPases Rap1 and Rap2 in response to intracellular cAMP. EPAC2 is mainly expressed in the central nervous system, pancreas and adrenal gland [1].
HJC 0350 is a potent and selective EPAC2 antagonist. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 μM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 μM. In the presence of 25 μM cAMP, HJC 0350 (25 μM) inhibited EPAC2 GEF activity but had no effect on EPAC1-mediated Rap1-GDP exchange activity and cAMP-mediated PKA activation, which suggested that HJC 0350 was EPAC2-specific antagonist. In HEK293 cells expressing EPAC1- or EPAC2-based fluorescence resonance energy transfer (FRET) sensor (EPAC2-FL or EPAC1-FL), HJC 0350 (10 μM) completely inhibited the 007-AM (a membrane permeable EPAC selective cAMP analogue) induced decrease of FRET in HEK293/EPAC2-FL cells but had no effect on HEK293/EPAC1-FL cells [1].
Reference:
[1]. Chen H, Tsalkova T, Chepurny OG, et al. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem, 2013, 56(3): 952-962.
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Identification and characterization of small molecules as potent and specific EPAC2 antagonists.[Pubmed:23286832]
J Med Chem. 2013 Feb 14;56(3):952-62.
EPAC1 and EPAC2, two isoforms of exchange proteins directly activated by cAMP (EPAC), respond to the second messenger cAMP and regulate a wide variety of intracellular processes under physiological and pathophysiological circumstances. Herein, we report the chemical design, synthesis, and pharmacological characterization of three different scaffolds (diarylsulfones, N,N-diarylamines, and arylsulfonamides) as highly potent and selective antagonists of EPAC2. Several selective EPAC2 antagonists have been identified including 20i (HJC0350), which has an apparent IC(50) of 0.3 muM for competing with 8-NBD-cAMP binding of EPAC2 and is about 133-fold more potent than cAMP. Compounds 1 (ESI-05), 14c (HJC0338), and 20i, selected from each series, have exhibited no inhibition of EPAC1-mediated Rap1-GDP exchange activity at 25 muM, indicating that they are EPAC2-specific antagonists. Moreover, live-cell imaging studies using EPAC1, EPAC2, or PKA FRET sensor also demonstrate that 20i functions as an EPAC2 specific antagonist.
