FR 180204

Research use only, not for human use.

FR 180204 is a potent, selective, ATP-competitive ERK inhibitor with Ki of 0.31 and 0.14 uM for ERK1 and ERK2, respectively.

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.

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.

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.

FR180204 | FR-180204

MAPK/ERK Signaling

ERK

ERK1|ERK2

Cancer

——

865362-74-9

327.3427

C18H13N7

>98% (HPLC)

DMSO: ≥ 50 mg/mL

NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21

1H-Pyrazolo[3,4-c]pyridazin-3-amine, 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-

(-20℃)

With Ice Pack

≥ 2 years