产品说明书

FR 180204

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Chemical Structure| 865362-74-9 同义名 : ERK Inhibitor II
CAS号 : 865362-74-9
货号 : A867944
分子式 : C18H13N7
纯度 : 98%
分子量 : 327.343
MDL号 : MFCD14585805
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(152.75 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • ERK2

    ERK2, Ki:0.14 μM

  • ERK1

    ERK1, Ki:0.31 μM
描述 The extracellular signal-regulated kinase (ERK) pathway is a key signaling cascade involved in cell growth and proliferation. FR 180204 is a potent, selective ERK inhibitor that inhibits the kinase activity of ERK1 and ERK2 with IC50 values of 0.51 and 0.33 µM, respectively, and Ki values of 0.31 and 0.14 µM, respectively. FR 180204 also inhibits p38α with an IC50 value of 10 µM. FR180204 dose-dependently inhibited AP-1 transactivation in Mv1Lu cells with an IC50 of 3.1 µM[3]. Pretreatment of FR 180204 at 100 mg/kg (i.p., b.i.d.) significantly ameliorated the bodyweight loss and clinical arthritis in mice with collagen-induced arthritis (CIA). CIA mice treated with FR 180204 also showed a reduction (62%) in the plasma level of anti-type II collagen (CII) compared to the control group. In CII-immunized DBA/1 mice, FR 180204 (32 and 100mg/kg) decreased delayed-type hypersensitivity induced by CII-reactive T cells in a dose-dependent manner. It also inhibited in vitro CII-induced proliferation of lymph node cells prepared from CII-immunized mice[4].
作用机制 FR 180204 selectively inhibits ERK1/2 in an ATP-competitive manner. The novel hydrophobic interactions in FR180204/ERK complex attribute to the selectivity and potency of FR180204.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.31mL

15.27mL

3.05mL

1.53mL

30.55mL

6.11mL

3.05mL
参考文献

[1]Honda M, Kanno T, et al. Mesothelioma cell proliferation through autocrine activation of PDGF-ββ receptor. Cell Physiol Biochem. 2012;29(5-6):667-74.

[2]Ohori M, Kinoshita T, et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63.

[3]Ohori M, Kinoshita T, Okubo M, Sato K, Yamazaki A, Arakawa H, Nishimura S, Inamura N, Nakajima H, Neya M, Miyake H, Fujii T. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63. doi: 10.1016/j.bbrc.2005.08.082. PMID: 16139248.

[4]Ohori M, Takeuchi M, Maruki R, Nakajima H, Miyake H. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6. doi: 10.1007/s00210-006-0117-7. Epub 2006 Nov 23. PMID: 17123065.