An allosteric inhibitor of MEK1
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PD 318088

Item No. 30265

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
CAS Number
391210-00-7
Molecular Formula
C16H13BrF3IN2O4
Formula Weight
561.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/mlEthanol: 1 mg/ml
λmax
239, 284 nm
SMILES
BrC1=C(F)C(F)=C(NC2=C(F)C=C(I)C=C2)C(C(NOCC(O)CO)=O)=C1
InChi Code
InChI=1S/C16H13BrF3IN2O4/c17-10-4-9(16(26)23-27-6-8(25)5-24)15(14(20)13(10)19)22-12-2-1-7(21)3-11(12)18/h1-4,8,22,24-25H,5-6H2,(H,23,26)
InChi Key
XXSSGBYXSKOLAM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $376

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    25 mg

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    Product Description

    PD 318088 is an allosteric inhibitor of MEK1 and an analog of the MEK inhibitor PD 184352 (CI-1040; Item No. 11580).1,2 PD318088 binds to MEK1 concurrently with Mg-ATP and stabilizes an inactive conformation of MEK1, as well as prevents formation of tetramers and higher-order oligomers.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ohren, J.F., Chen, H., Pavlovsky, A., et al. Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat. Struct. Mol. Biol. 11(12), 1192-1197 (2004).

    2. Shang, J., Lu, S., Jiang, Y., et al. Allosteric modulators of MEK1: Drug design and discovery. Chem. Biol. Drug Des. 88(4), 485-497 (2016).