A potent MEK5 inhibitor
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BIX02188

Item No. 16238

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3Z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide
CAS Number
334949-59-6
Molecular Formula
C25H24N4O2
Formula Weight
412.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
210, 285, 384 nm
SMILES
CN(C)CC1=CC(N/C(C2=CC=CC=C2)=C3C(NC4=C\3C=CC(C(N)=O)=C4)=O)=CC=C1
InChi Code
InChI=1S/C25H24N4O2/c1-29(2)15-16-7-6-10-19(13-16)27-23(17-8-4-3-5-9-17)22-20-12-11-18(24(26)30)14-21(20)28-25(22)31/h3-14,27H,15H2,1-2H3,(H2,26,30)(H,28,31)/b23-22-
InChi Key
FSZPIAXLCCQFCM-FCQUAONHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $178

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    10 mg

    $306

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    25 mg

    $645

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    Product Description

    BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFβR1 (IC50s = 810 and 1,800 nM, respectively).1 It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM).1 BIX02188 inhibits phosphorylation of ERK5 in a dose-dependent manner without affecting phosphorylation of ERK1/2, p38 MAPK, or JNK1/2.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tatake, R.J., O'Neill, M.M., Kennedy, C.A., et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem. Biophys. Res. Commun. 377(1), 120-125 (2008).