HJC0197 |
| Catalog No.GC17072 |
Epac1 and Epac2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1383539-73-8
Sample solution is provided at 25 µL, 10mM.
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HJC0197 is a cell-permeable inhibitor of Epac1 and Epac2.
Exchange proteins directly activated by cAMP (Epac) are Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMP implicated in regulating a wide variety of intracellular processes in response to second messenger cAMP [1].
In vitro: HJC0197 showed an inhibitory effect against Epac2 with an IC50 value of 5.9 μM. In the presence of equal concentration of cAMP, HJC0197 inhibited Epac2 GEF activity to basal levels at 25 μM. HJC0197 also inhibited Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP. HJC0197 was Epac-specific inhibitors that selectively blocked cAMP-induced Epac activation, but didn’t inhibit cAMP-mediated PKA activation. In HEK293/Epac1 and HEK293/Epac2 cells, pretreatment of with 10 μM HJC0197 for 5 min before the administration of 007-AM, a membrane permeable Epac selective agonist, completely blocked Epac1 and Epac2-mediated Akt phosphorylation [2]. In chicken micromass cultures, inhibition of the PKA-independent cAMP-mediators Epac1 and Epac2 with HJC0197 enhanced cartilage formation [3].
References:
[1]. De Rooij J, Zwartkruis F J T, Verheijen M H G, et al. Epac is a Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMP[J]. Nature, 1998, 396(6710): 474-477.
[2]. Chen H, Tsalkova T, Mei F C, et al. 5-Cyano-6-oxo-1, 6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP[J]. Bioorganic & medicinal chemistry letters, 2012, 22(12): 4038-4043.
[3]. Juhász T, Matta C, Somogyi C, et al. Mechanical loading stimulates chondrogenesis via the PKA/CREB-Sox9 and PP2A pathways in chicken micromass cultures [J]. Cellular signaling, 2014, 26(3): 468-482.
| Cas No. | 1383539-73-8 | SDF | |
| Chemical Name | 4-cyclopentyl-2-[[(2,5-dimethylphenyl)methyl]thio]-1,6-dihydro-6-oxo-5-pyrimidinecarbonitrile | ||
| Canonical SMILES | CC(C=CC(C)=C1)=C1CSC(NC(C2CCCC2)=C3C#N)=NC3=O | ||
| Formula | C19H21N3OS | M.Wt | 339.5 |
| Solubility | ≤5mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9455 mL | 14.7275 mL | 29.4551 mL |
| 5 mM | 0.5891 mL | 2.9455 mL | 5.891 mL |
| 10 mM | 0.2946 mL | 1.4728 mL | 2.9455 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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