An inhibitor of MEK5 and ERK5
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BIX02189

Item No. 16999

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3Z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
CAS Number
1265916-41-3
Molecular Formula
C27H28N4O2
Formula Weight
440.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
284, 385 nm
SMILES
CN(C)CC1=CC(N/C(C2=CC=CC=C2)=C3C(NC4=C\3C=CC(C(N(C)C)=O)=C4)=O)=CC=C1
InChi Code
InChI=1S/C27H28N4O2/c1-30(2)17-18-9-8-12-21(15-18)28-25(19-10-6-5-7-11-19)24-22-14-13-20(27(33)31(3)4)16-23(22)29-26(24)32/h5-16,28H,17H2,1-4H3,(H,29,32)/b25-24-
InChi Key
HOMJAAIVTDVQJA-IZHYLOQSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $129

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    10 mg

    $231

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    25 mg

    $319

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    Product Description

    BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C.1 It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2.1 BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells.1 It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.2,3

    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).

    2. Obara, Y., and Nakahata, N. The signaling pathway leading to extracellular signal-regulated kinase 5 (ERK5) activation via G-proteins and ERK5-dependent neurotrophic effects. Mol. Pharmacol. 77(1), 10-16 (2010).

    3. Wang, X., Pesakhov, S., Weng, A., et al. ERK 5/MAPK pathway has a major role in 1a,25-(OH)2 vitamin D3-induced terminal differentiation of myeloid leukemia cells. J. Steroid Biochem. Mol. Biol. 144(Pt. A), 223-227 (2014).