ESI-08

ESI-08 是一种有效的选择性 EPAC 拮抗剂，可以完全抑制 EPAC1 和 EPAC2 (IC50 为 8.4 μM) 的活性。ESI-08 选择性阻断 cAMP 诱导的 EPAC 激活，但不抑制 cAMP 介导的 PKA 激活。

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库存: 现货

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促销价

数量
5mg

￥1462.00

1170.00

- +
10mg

￥2437.00

1950.00

- +
25mg

￥5337.00

4270.00

- +
50mg

￥8250.00

6600.00

- +
100mg

￥12975.00

10380.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajcf14674
CAS: 301177-43-5
别名:
分子式: C20H23N3OS
分子量: 353.48
纯度: >98%
溶解度: DMSO : 100 mg/mL (282.90 mM; ultrasonic and warming and heat to 60°C)
储存: 4°C, protect from light
库存: 现货

Background

IC50: 8.4 μM (EPAC2)^[1]
EPAC1^[1]

ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC₅₀ of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation^[1].

Exchange proteins directly activated by cAMP (EPAC) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes in response to second messenger cAMP. ESI-08 at 25 μM has been found not to alter cAMP-induced type I and II PKA holoenzymes activation while H89, a selective PKA inhibitor, blocked the type I or II PKA activities completely^[1].