A MEK5 inhibitor
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MEK Inhibitor

Item No. 43190

Technical Information
Formal Name
(3Z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N-methyl-2-oxo-1H-indole-6-carboxamide
CAS Number
334951-92-7
Synonyms
  • BIX02189
Molecular Formula
C26H26N4O2
Formula Weight
Purity
≥95%
A solid
DMSO: Soluble: ≥ 10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N1)/C(C(C1=C2)=CC=C2C(NC)=O)=C(C3=CC=CC=C3)\NC4=CC(CN(C)C)=CC=C4
InChi Code
InChI=1S/C26H26N4O2/c1-27-25(31)19-12-13-21-22(15-19)29-26(32)23(21)24(18-9-5-4-6-10-18)28-20-11-7-8-17(14-20)16-30(2)3/h4-15,28H,16H2,1-3H3,(H,27,31)(H,29,32)/b24-23-
InChi Key
BQNHHYZMVCQLJG-VHXPQNKSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MEK inhibitor is an inhibitor of MEK5 (IC50 = 1.5 nM).1 It is selective for MEK5 over ERK5, activin receptor-like kinase 5 (ALK5), also known as TGF-β receptor type I (TGF-βRI), MEK1, and MEK2 (IC50s = 59, 580, >6,300, and >6,300 nM, respectively) and a panel of 79 other kinases at 10 µM. MEK inhibitor (1, 3, or 10 µM) decreases the levels of phosphorylated ERK5 in sorbitol-stimulated HeLa cells. It inhibits TGF-β1-induced increases in N-cadherin levels, decreases in E-cadherin levels, and cell migration in a scratch assay in A549 lung cancer cells when used at a concentration of 10 µM.2 MEK inhibitor (20 mg/kg per day) decreases the number of lung nodules in an A549 mouse model of lung metastasis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Park, S.J., Choi, Y.S., Lee, S., et al. BIX02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor. Cancer Lett. 381(2), 314-322 (2016).