CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of one of the key components of this pathway (MEK1/MEK2), and thereby effectively blocks the phosphorylation of ERK and continued signal transduction through this pathway.
|Cell lines||CCl39 cells expressing FLAG-ERK5|
|Preparation method||Cells were serum-starved for 16 h prior to the addition of PD184352, or an equivalent of DMSO vehicle control for 90 min. Single dishes of cells were then stimulated with 10% FBS for 15 min and immune-complex kinase assays performed with either myelin basic protein (MBP; ERK1) or GST-MEF2C (ERK5), as a substrate. PD184352 inhibited FBS-induced ERK1 activation with an IC50 below 1 μM, whereas even a dose of 20 μM PD184352 was insufficient to inhibit ERK5 activity, induced in the same manner and assayed from the same cell extracts as ERK1.|
|Animal models||DBA/2-pcy/pcy mice|
|Dosages||400 mg/kg daily for the first week and then every third day for 6 additional weeks|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Inhibition of MEK pathway in vestibular schwannoma cell culture.
Neff et al. Laryngoscope. 2012 Aug 10. PMID: 22886786.
The MEK inhibitor PD184352 enhances BMS-214662-induced apoptosis in CD34+ CML stem/progenitor cells.
Pellicano et al. Leukemia. 2011 Jul;25(7):1159-67. PMID: 21483442.
|Related MEK Products|
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively.
|AZD6244 sulfate salt|
LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase (MEK1/2).
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