ESI-09 263707-16-0

簡要描述：ESI-09 263707-16-0
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.

產(chǎn)品型號：abs47027962
廠商性質(zhì)：生產(chǎn)廠家
更新時間：2026-01-09
訪問量：638

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品牌	absin	CAS	263707-16-0
分子式	C16H15ClN4O2	純度	＞98%
分子量	330.77	貨號	abs47027962
規(guī)格	5mg	供貨周期	現(xiàn)貨
主要用途	is a specific exchange protein	應(yīng)用領(lǐng)域	化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合

ESI-09 263707-16-0

產(chǎn)品描述
描述	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.
純度	＞98%
儲存/保存方法	Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
別名	ESI 09
外觀	faint yellow to dark orange powder
可溶性/溶解性	DMSO : 33.1 mg/mL (100 mM) Ethanol : 6.6 mg/mL (20 mM)
生物活性
靶點(diǎn)	EPAC2 ,EPAC1
In vitro(體外研究)	ESI-09, a novel non-cyclic 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. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves.
In vivo(體內(nèi)研究)	ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis.
參考文獻(xiàn)
參考文獻(xiàn)	1. Almahariq M , et al. Mol Pharmacol. 2013, 83(1), 122-128. 2. Gong B, et al. Proc Natl Acad Sci U S A. 2013, 110(48), 19615-19620.

研究領(lǐng)域
研究領(lǐng)域	Signal TransductionSecond MessengerNucleotide MessengercAMP Signal TransductionSecond MessengerNucleotide MessengercGMP Drug DiscoverySmall Molecule DrugLead Compound Discovery

ESI-09 263707-16-0溫馨提示：本產(chǎn)品僅作科研實(shí)驗(yàn)使用，不支持臨床等研究

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上一篇：abs47027961GSK2578215A 1285515-21-0
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ESI-09 263707-16-0

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