Tocris Bioscience
 Welcome to Tocris

| Advanced Search
Home Products Technical Support Customer Support Literature Custom Synthesis
Category: EnzymesarrowKinasesarrowMAPK/MAPKK
Cat.No. Product Name
2605 PD 198306
Price and Availability

Click here for full price details of
PD 198306
Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-met hylphenyl)amino]-benzamide

Biological Activity:

Potent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30-100 nM. Highly selective for MEK; IC50 values are > 1, > 4, > 4 and > 10 μM for ERK, c-Src, cdks and PI 3-kinase γ respectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.

Technical Data:

 Click here for more information on batch specific data
M.Wt: 476.23
Formula: C18H16F3IN2O2
Storage: Store at +4°C
Solubility: Soluble to 100 mM in DMSO and to 100 mM in Ethanol
Purity: >98%
CAS No: [212631-61-3]

Resources:

    		•

    • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Ciruela et al (2003) Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br.J.Pharmacol. 138 751. Pelletier et al (2003) In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthrit.Rheumat. 48 1582.
    View related products by Pharmacological Action or by Research Area

    Keywords: PD 198306, Kinases, Selective Inhibitor Of MEK1 / 2, PD198306, Tocris Bioscience
    Literature in this Area
    Scientific Reviews
    Function & Modulation of MAP Kinase Pathways
    Download PDF
    Signal Transduction Guide
    Signal Transduction Guide : An informative guide for all scientists working in: Cell cycle & apoptosis, Protein kinases & phosphatases, Ion channels, Calcium & lipid signaling, Cyclic nucleotides & G-proteins, Nitric oxide, & Signaling EnzymesA complete listing of signal transduction products available from Tocris, including descriptions on selected tools and unit sizes.
    View PDF
    Product Feature
    cMet Signalling
    Key cMet signalling compounds available from Tocris include:
    2693   PHA 665752
    Potent and selective cMET inhibitor
    1683   K 252a
    Receptor tyrosine kinase inhibitor
    1130   LY 294002
    Selective PI 3-Kinase inhibitor
    2605   PD 198306
    Selective inhibitor of MEK1/2
    2798   Stattic
    Selective STAT3 inhibitor
    View Product Feature
    New Products in this Area

     2930PI 103 hydrochloride
     Inhibitor of PI 3-kinase, mTOR and DNA-PK
     3028Rp-8-Br-PET-cGMPS
     Protein kinase G inhibitor
     2992PKC 412
     Protein kinase C inhibitor
     2977GW 843682X
     Selective inhibitor of PLK1 and PLK3
     2828NU 7026
     Selective DNA-dependent protein kinase inhibitor
     2938SD 169
     Selective, orally active p38α inhibitor
     2910H 89 dihydrochloride
     Protein kinase A inhibitor
     2864Metformin hydrochloride
     Activator of LKB1/AMPK; antidiabetic agent
     2877MNS
     Selective inhibitor of Src and Syk
     2794PP 3
     Negative control for PP 2 (Cat. No. 1407)
     2755DCA
     Mitochondrial pyruvate dehydrogenase kinase (PDK) inhibitor
     1571Cucurbitacin I
     Selective inhibitor of STAT3/JAK2 signalling
     2731CGP 57380
     Selective inhibitor of Mnk1
     1626Calphostin C
     Potent, selective and photo-dependent PKC inhibitor
     2253Go 6976
     Potent protein kinase C inhibitor; selective for α and β isozymes
     2560SB 218078
     Inhibitor of checkpoint kinase 1 (Chk1)
     2539IKK 16
     Selective inhibitor of IKK
     2605PD 198306
     Selective inhibitor of MEK1/2
     2651AEG 3482
     Inhibitor of JNK signalling
     2639CGK 733
     Selective inhibitor of ATR and ATM kinases
     2609Ryuvidine
     Cyclin-dependent kinase 4 (cdk4) inhibitor
     2694PD 407824
     Selective inhibitor of Chk1 and Wee1
     1587Ro 32-0432 hydrochloride
     Potent, orally active PKC inhibitor
     2285Go 6983
     Broad spectrum PKC inhibitor
     2485Glycyl-H 1152 dihydrochloride
     More selective analogue of Cat. No. 2414
     2559TPCA-1
     Potent, selective inhibitor of IKK-2
     2611IMD 0354
     Inhibitor of IKK-2
     2657JX 401
     Potent, reversible p38α inhibitor
     2414H 1152 dihydrochloride
     Selective rho-kinase (ROCK) inhibitor
     2287K-252c
     Protein kinase C inhibitor
     255810-DEBC hydrochloride
     Selective Akt/PKB inhibitor
     2549ZIP
     Cell-permeable inhibitor of atypical PKC isozyme PKMz
     2383Bryostatin 1
     Protein kinase C activator
     2357Anti-Cdk2
     Antibody recognising Cdk2
     2367Anti-PKC
     Antibody recognising PKC
     2356Anti-Cdk1 and Cdk2
     Antibody recognising Cdk1 and Cdk2
     2358Anti-c-Jun
     Antibody recognising c-Jun
     2243MEK Inhibitor TocrisetTM
     Selection of 3 MEK inhibitors (Cat. Nos. 1213, 1969 and 1144)
     2244p38 MAPK Inhibitor TocrisetTM
     Selection of 3 p38 MAPK inhibitors (Cat. Nos. 1264, 1202 and 1962)
    Sign-up for new product e-alerts
    Log In / Register

    User ID
    Password
    If you are not registered with us Create Account
    Home | About | Contact | Environment | Distributors | Glossary | Ordering | Security | Privacy | Terms & Conditions | Services | Site Map