FR 180204

SKU: orb1223814

Description

FR 180204 is a potent, selective, ATP-competitive ERK inhibitor with Ki of 0.31 and 0.14 uM for ERK1 and ERK2, respectively; inhibits TGFβ-induced luciferase-expression in mink lung epithelial Mv1Lu cells, decreases plasma anti-CII antibody levels and attenuates delayed-type hypersensitivity in CII-immunized DBA/1 mice, also inhibits in vitro CII-induced proliferation of lymph node cells prepared from CII-immunized mice; enhances apoptotic and anti-proliferative effects of Akt inhibitor API-1 in human DLD-1 and LoVo colorectal cancer cells.

Key Properties

• CAS Number: 865362-74-9
• MW: 327.3427
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃N₇
• SMILES: NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21
• Target: ERK
• Solubility: DMSO: ≥ 50 mg/mL

Bioactivity

• In Vivo:
  FR180204 (100 mg/kg, i.p. , b. i. d.) significantly decreases the severity of symptoms and body weight loss in collagen-induced arthritis mice. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves clinical parameters.
• In Vitro:
  In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM. FR 180204 inhibits spontaneous mesothelioma cell growth.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FR180204 | FR-180204

Quick Database Links

Gene Symbol

ERK