865362-74-9|FR 180204|CsnPharm

CAS No.: 865362-74-9

FR 180204 Catalog No. CSN13064

Synonyms: ERK Inhibitor II

FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2 with Ki value of 0.31 μM and 0.14 μM respectively and has IC50 values of 0.51 and 0.33 μM in enzymatic assays against ERK1 and ERK2, respectively.

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技术信息

生物活性

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 K_i 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.
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0549 mL
- 15.2745 mL
- 30.5490 mL
- 5 mM
- 0.6110 mL
- 3.0549 mL
- 6.1098 mL
- 10 mM
- 0.3055 mL
- 1.5275 mL
- 3.0549 mL

技术信息

CAS号

865362-74-9

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H13N7

运输

蓝冰

分子量

327.34

别名

ERK Inhibitor II

溶解度

DMSO	64.0 mg/mL (195.5 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (6.1 mM) warming

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