Chemical Properties
Off-White to Pale Beige Solid
Uses
An inhibitor of ERK signaling pathway. A MAP kinase inhibitor
Definition
ChEBI: 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide is an aminobenzoic acid.
Biological Activity
Potent and selective inhibitor of MAPK (ERK kinase 1; MEK1) activation (IC50=300nM in vitro, IC50=2nM in vivo). Suppresses activation of MAPK but does not block its activity. Strongly suppresses growth of human implanted colon tumors in mice.
Biochem/physiol Actions
PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.
Enzyme inhibitor
This substituted benzamide (FW = 478.66 g/mol), also known as 2- (chloro-
4-iodophenylamino) -N-cyclopropylmethoxy-3,4-difluorobenzamide and CI-
1040, inhibits ERK activation, IC50 = 16 nM.
References
[1] frémin c, meloche s. from basic research to clinical development of mek1/2 inhibitors for cancer therapy. j hematol oncol. 2010 feb 11;3:8. doi: 10.1186/1756-8722-3-8.
