FR180204

• CAT Number: I005200
• CAS Number: 865362-74-9
• Molecular Formula: C₁₈H₁₃N₇
• Molecular Weight: 327.34
• Purity: ≥95%
• Synonyms: 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine
• Target: ERK
• Solubility: DMSO: ≥ 50 mg/mL
• Storage: 2-8°C
• IC50: 0.31 uM/0.14 uM(Ki for ERK1/ERK2); 0.51uM/0.33 μM(ERK1/ERK2)
• IUPAC Name: 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-2H-pyrazolo[3,4-c]pyridazin-3-amine
• InChI: InChI=1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
• InChIKey: XVECMUKVOMUNLE-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)C2=NN3C=CC=CC3=C2C4=CC5=C(NN=C5N=N4)N

FR180204（Cat No.:I005200）is a highly potent and selective inhibitor of ERK1 and ERK2, two enzymes involved in the MAPK/ERK signaling pathway. It competitively binds to the ATP-binding site of ERK1 and ERK2, effectively inhibiting their activity. With a Ki value of 0.31 μM and 0.14 μM for ERK1 and ERK2, respectively, and IC50 values of 0.51 μM and 0.33 μM in enzymatic assays, FR180204 demonstrates strong inhibitory effects on these kinases, making it a valuable tool for studying the MAPK/ERK signaling pathway and its associated cellular processes.

Reference

[1]. Ohori M, 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.
[2]. Aronov AM, et al. Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors. J Med Chem. 2007 Mar 22;50(6):1280-7.
[3]. Ohori M, et al. 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.