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BIX 02189

BIX 02189

Catalog Number:
L002369361APE
Mfr. No.:
APE-A5801
Price:
$289
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      • Overview

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          Background

          BIX 02189 is a selective inhibitor of MEK5 with IC50 value of 1.5 nM 1.
          BIX 02189 belongs to the indolinone kinase inhibitor series. It selectively inhibited the catalytic activity of MEK5 but not other closely related kinases such as MEK1, MEK2, ERK2 and JNK2. BIX 02189 also inhibited ERK5 with IC50 value of 59 nM. In HeLa cells, treatment of BIX 02189 inhibited the phosphorylation of ERK5 but not ERK1/2. Besides that, BIX 02189 prevented the transcription of the downstream substrate MEF2C in HeLa and HEK293 cells. Moreover, in a three-dimensional lymphangiogenic sprouting assay, BIX 02189 resulted in an inhibition of lymphangiogenic sprouting with a minimal effective concentration of 1 μM 1,2.

          1. Tatake R J, O’Neill M M, Kennedy C A, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochemical and biophysical research communications, 2008, 377(1): 120-125.
          2. Schulz M M P, Reisen F, Zgraggen S, et al. Phenotype-based high-content chemical library screening identifies statins as inhibitors of in vivo lymphangiogenesis. Proceedings of the National Academy of Sciences, 2012, 109(40): E2665-E2674.

      • Properties
        • Alternative Name
          (3Z)-3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide
          CAS Number
          1094614-85-3
          Molecular Formula
          C27H28N4O2
          Molecular Weight
          440.54
          Appearance
          A solid
          Purity
          99.13%
          Solubility
          ≥22.05 mg/mL in DMSO; insoluble in H2O; ≥40.7 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

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