Pular para o conteúdo
Merck
Todas as fotos(1)

Key Documents

SML2355

Sigma-Aldrich

BIX02189

≥98% (HPLC)

Sinônimo(s):

(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

Faça loginpara ver os preços organizacionais e de contrato


About This Item

Fórmula empírica (Notação de Hill):
C27H28N4O2
Número CAS:
Peso molecular:
440.54
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

−20°C

cadeia de caracteres SMILES

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-

chave InChI

HOMJAAIVTDVQJA-IZHYLOQSSA-N

Ações bioquímicas/fisiológicas

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.).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

Já possui este produto?

Encontre a documentação dos produtos que você adquiriu recentemente na biblioteca de documentos.

Visite a Biblioteca de Documentos

Revati J Tatake et al.
Biochemical and biophysical research communications, 377(1), 120-125 (2008-10-07)
We have identified two novel MEK5 inhibitors, BIX02188 and BIX02189, which inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. The compounds also inhibited transcriptional activation
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
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
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)
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

Nossa equipe de cientistas tem experiência em todas as áreas de pesquisa, incluindo Life Sciences, ciência de materiais, síntese química, cromatografia, química analítica e muitas outras.

Entre em contato com a assistência técnica