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Documentos

SML2355

Sigma-Aldrich

BIX02189

≥98% (HPLC)

Sinónimos:

(3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide, (Z)-3-((3-((Dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide, BIX 02189, BIX-02189

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About This Item

Fórmula empírica (notación de Hill):
C27H28N4O2
Número de CAS:
1265916-41-3
Peso molecular:
440.54
MDL number:
MFCD18074528
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

CN(C)CC1=CC=CC(N/C(C2=CC=CC=C2)=C(C3=CC=C(C(N(C)C)=O)C=C3N4)\C4=O)=C1

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

Biochem/physiol Actions

BIX02189 is an ATP site-targeting, potent and selective MEK5 inhibitor (IC50 =1.5 nM, [ATP] = 750 nM) with much reduced or no potency against 79 other kinases (CSF1R (FMS)/ERK5/Lck/Jak3/TGFβR1/RPS6KA6 (RSK4) IC50 = 46/59/250/440/580/990 nM, MEK1/MEK2/ERK2/JNK2/EGFR/STK16 IC50 >6.2 μM). BIX02189 blocks cellular ERK5, but not ERK1/2 or p38, phosphorylation induction (IC50 <1 μM in sorbitol-stimulated HeLa), as well as downstream MEF2C transcriptional activation (IC50 = 0.53/0.26 μM, MEK5/ERK5/MEF2C HeLa/HEK293 reporter cells). BIX02189 in vivo efficacies are demonstrated in murine models of atherosclerosis, cancer, and diabetes (10-20 mg/kg i.p.).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Qi Zhao et al.
Oncotarget, 9(1), 1229-1236 (2018-02-09)
Diabetic retinopathy (DR) is a major complication of diabetes, and causes pathological changes in retina blood vessels, as the most common cause of vision loss. Extracellular-signal-regulated kinase 5 (ERK5) is the newest discovered member in the mitogen-activated protein kinases (MAPKs)
Seong Ji Park et al.
Cancer letters, 381(2), 314-322 (2016-08-21)
Transforming growth factor-β1 (TGF-β1) promotes tumor metastasis by inducing an epithelial-to-mesenchymal transition (EMT) in cancer cells. In this study, we investigated the effects of BIX02189 and XMD8-92, pharmacologic inhibitors of the MEK5 [mitogen-activated protein kinase/extracellular-signal-regulated kinase (ERK)5] signaling pathway, on
Congde Chen et al.
Cell proliferation, 51(3), e12410-e12410 (2017-11-22)
Restoring a functional beta-cell mass is a fundamental goal in treating diabetes. A complex signalling pathway network coordinates the regulation of beta-cell proliferation, although a role for ERK5 in this network has not been reported. This question was addressed in
Huang-Joe Wang et al.
Frontiers in physiology, 8, 1095-1095 (2018-01-23)
Background and Aims: Endothelial dysfunction is a hallmark of cardiovascular diseases. The straight region of an artery is protected from atherosclerosis via its laminar blood flow and high shear stress. This study investigated the cytoprotective effects of a new laminar
Carolyn J Loveridge et al.
Scientific reports, 7(1), 13241-13241 (2017-10-19)
Extracellular signal-regulated protein kinase 5 (ERK5) has been implicated during development and carcinogenesis. Nkx3.1-mediated Cre expression is a useful strategy to genetically manipulate the mouse prostate. While grossly normal at birth, we observed an unexpected phenotype of spinal protrusion in
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