An orally bioavailable and potent inhibitor of MEK1/2 inhibitor (IC50 = 8 nM); selective for MEK1/2 over ERK

PD 198306 – 5 mg

Brand:
Cayman
CAS:
212631-61-3
Storage:
-20
UN-No:
Non-Hazardous - /

PD 198306 is an orally bioavailable and potent inhibitor of MAPK kinase 1/2 (MEK1/2; IC50 = 8 nM).{38577} It is selective for MEK1/2 over ERK, c-Src, PI3Kγ, and cyclin-dependent kinases (IC50s = >1 μM). PD 198306 (3-100 μM) reduces ERK1/2 phosphorylation and inhibits growth of HL-60 cells in vitro.{38578} In vivo, PD 198306 (10-30 mg/kg) reduces ERK1/2 phosphorylation and matrix metalloproteinase-1 (MMP-1) expression in a dose-dependent manner in a rabbit model of osteoarthritis.{38577} It also reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of neuropathic pain induced by streptozotocin (Item No. 13104) or chronic constriction injury.{38579}  

 

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SKU: 23966 - 5 mg Category:

Description

An orally bioavailable and potent inhibitor of MEK1/2 inhibitor (IC50 = 8 nM); selective for MEK1/2 over ERK, c-Src, PI3Kγ, and cyclin-dependent kinases (IC50s = >1 μM); reduces ERK1/2 phosphorylation and inhibits growth of HL-60 cells in vitro; reduces ERK1/2 phosphorylation and MMP-1 expression in a dose-dependent manner in a rabbit model of osteoarthritis when administered at doses ranging from 10-30 mg/kg; reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of streptozotocin- and chronic constriction injury-induced neuropathic pain,

Formal name: N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide

Synonyms: 

Molecular weight: 476.2

CAS: 212631-61-3

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Neuroscience|Pain Research

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