PD184352 (CI-1040)

Short Summary : Selective MEK inhibitor

Category : MAPK Signaling|MEK1/2

Purity : 0.9982

CAS Number : 212631-79-3

Formula : C17H14ClF2IN2O2

Molecular Weight : 478.67

SMILE : C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl

Solubility : >47.9mg/mL in DMSO

Storage : Store at -20°C

Description : PD184352 (also known as CI-1040), a benzhydroxamate derivative, is a potent and highly selective MEK1/2, two members of the family of MAPKKs, inhibitor that inhibits purified MEK1 with IC50 of 17 nM in a non-ATP and non-ERK1/2 competitive manner [1]. PD184352 binds to a hydrophobic pocket, which is located in a region with low sequence homology to other kinases, adjacent to the Mg-ATP binding site of MEK1 and MEK2 inducing a conformational change in un-phosphorylated MEK1/2 and hence inactivating the un-phosphorylated MEK1/2 [1]. PD184352 has been found to be actively against tumors, where it inhibits the growth of colon carcinomas in mouse xenograft models [1].References:[1] Frmin 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.

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