HJC0197
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 339.5 |
Cas No. | 1383539-73-8 |
Formula | C19H21N3OS |
Solubility | ≤5mg/ml in DMSO;10mg/ml in dimethyl formamide |
Chemical Name | 4-cyclopentyl-2-[[(2,5-dimethylphenyl)methyl]thio]-1,6-dihydro-6-oxo-5-pyrimidinecarbonitrile |
SDF | Download SDF |
Canonical SMILES | CC(C=CC(C)=C1)=C1CSC(NC(C2CCCC2)=C3C#N)=NC3=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |