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PD318088

Cat. No. M1905
PD318088 Structure
Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 260 In stock
50mg USD 790 In stock
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Biological Activity

PD318088 is a novel, small-molecule inhibitor of MEK1/2. MEK1 and MEK2 are closely related, dual-specificity tyrosine/threonine protein kinases found in the Ras/Raf/MEK/ERK mitogen-activated protein kinase (MAPK) signaling pathway. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 induces several conformational changes in the unphosphorylated MEK1 and MEK2 enzymes that lock them into a closed but catalytically inactive species.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 561.09
Formula C16H13BrF3IN2O4
CAS Number 391210-00-7
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.
Ohren JF, et al. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. PMID: 15543157.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PD318088 supplier, MEK, inhibitors

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