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263707-16-0
  • names:

    ESI-09

  • CAS號(hào):

    263707-16-0

    MDL Number: MFCD00109218
  • MF(分子式): C16H15ClN4O2 MW(分子量): 330.77
  • EINECS:No data available Reaxys Number:No data available
  • Pubchem ID:6077765 Brand:BIOFOUNT
ESI-09
ESI-09(263707-16-0)是一種新型非環(huán)狀核苷酸EPAC拮抗劑,能夠特異性阻斷細(xì)胞內(nèi)EPAC介導(dǎo)的Rap1活化和Akt磷酸化,以及EPAC介導(dǎo)的胰腺β細(xì)胞中胰島分泌。另一方面,ESI-09不抑制AsPC1細(xì)胞中表皮生長(zhǎng)因子(EGF)誘導(dǎo)的Akt磷酸化。在胰腺癌細(xì)胞中,ESI-09通過(guò)劑量依賴(lài)性降低007-AM誘導(dǎo)的細(xì)胞粘附而抑制細(xì)胞遷移和侵襲。ESI-09顯著降低人臍靜脈內(nèi)皮細(xì)胞中總細(xì)菌數(shù)。ESI-09有效拮抗CPT-cAMP誘導(dǎo)的Schwann細(xì)胞(SC)分化以及髓鞘的形成。在SC神經(jīng)元培養(yǎng)基中,ESI-09顯著降低O1陽(yáng)性和MBP陽(yáng)性的數(shù)量,而不影響神經(jīng)元或SCs自身的健康。
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中文別名 ESI-09(263707-16-0),ESI09,ESI 09
英文別名 ESI-09,263707-16-0,ESI09,ESI 09
CAS號(hào) 263707-16-0
Inchi InChI=1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+
InchiKey DXEATJQGQHDURZ-DEDYPNTBSA-N
分子式 Formula C16H15ClN4O2
分子量 Molecular Weight 330.77
溶解度Solubility 生物體外In Vitro:DMSO溶解度≥ 47 mg/mL(142.09 mM)H2O< 0.1 mg/mL(insoluble)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性狀 灰白色至橙色固體粉末
儲(chǔ)藏條件 Storage conditions 在-20°C條件下保存3年,在4°C條件下保存2年

ESI-09(263707-16-0)實(shí)驗(yàn)注意事項(xiàng):
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡,穿戴防護(hù)服和口罩,佩戴手套,避免與皮膚接觸。
2.實(shí)驗(yàn)過(guò)程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生,必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類(lèi)存儲(chǔ),并交于專(zhuān)業(yè)生物廢氣物處理公司處理,以免造成環(huán)境污染

ESI-09(263707-16-0)Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tag:ESI-09(263707-16-0),ESI-09抑制劑,ESI-09試劑,ESI-09的作用,ESI-09的純度,ESI-09雜質(zhì),ESI-09的外觀,ESI-09的溶解度,ESI-09的用途,ESI-09的合成,ESI-09的生產(chǎn),ESI-09的注意事項(xiàng),ESI-09的MSDS
產(chǎn)品說(shuō)明 ESI-09(263707-16-0)是一種新型非環(huán)狀核苷酸EPAC拮抗劑,能夠特異性阻斷細(xì)胞內(nèi)EPAC介導(dǎo)的Rap1活化和Akt磷酸化
IntroductionESI-09 (263707-16-0) is a new type of non-cyclic nucleotide EPAC antagonist, which can specifically block EPAC-mediated Rap1 activation and Akt phosphorylation in cells
Application1
Application2
Application3
ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.ESI-09 is a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. EPAC1 plays an important role in pancreatic cancer cell migration and invasion, and thus represents a potential target for developing novel therapeutic strategies for pancreatic cancer.
Role of Exchange Protein Directly Activated by Cyclic AMP Isoform 1 in Energy Homeostasis: Regulation of Leptin Expression and Secretion in White Adipose Tissue
Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC)
Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses
A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion
[Differences in the responses of taste receptors to organic and inorganic acids with changes in the concentration of bicarbonate in the solution]
Epac-inhibitors: facts and artefacts.
Rehmann H1. Sci Rep. 2013 Oct 23;3:3032. doi: 10.1038/srep03032.
cAMP is a universal second messenger. Its signalling is mediated by protein kinase A, Epac and certain types of ion channels in mammalians. cAMP signalling is involved in many physiological processes ranging from vision to the control of insulin secretion, pacemaker activity and gene transcription and therefore selective pharmacological interference is of medical interest. Whereas selective inhibitors of PKA and selective activators of Epac are well established, no inhibitors of Epac were available until recently. Here the action of four of the novel Epac inhibitors was analysed by biophysical means. ESI-05 is confirmed as a selective inhibitor of Epac2. No direct action of Brefeldin A on Epac could be demonstrated. ESI-09 and HJC0197 were found to act as chemicals with general protein denaturing properties and do not act on Epac selectively.
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