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Documentos Principais

SML0320

Sigma-Aldrich

FR180204

≥98% (HPLC)

Sinônimo(s):

5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine, 5-(2-Phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine, FR 180204

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About This Item

Fórmula empírica (Notação de Hill):
C18H13N7
Número CAS:
Peso molecular:
327.34
Número MDL:
Código UNSPSC:
12352200
ID de substância PubChem:
NACRES:
NA.77

Ensaio

≥98% (HPLC)

Formulário

powder

cor

faintly yellow to dark yellow

solubilidade

DMSO: ≥10 mg/mL

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

Nc1n[nH]c2nnc(cc12)-c3c(nn4ccccc34)-c5ccccc5

InChI

1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)

chave InChI

XVECMUKVOMUNLE-UHFFFAOYSA-N

Aplicação

FR180204 has been used as ERK inhibitor:
  • to block extracellular-signal-regulated kinase (ERK) in order to validate whether homeobox B7 (HOXB7) regulates the migration and proliferation process via AKT/mitogen-activated protein kinases (MAPK) signaling
  • of extracellular-signal-regulated kinase (ERK) to study the effects of signaling pathway inhibitors on differentiation and cell traction stress
  • to determine if phosphorylation of this signaling protein is essential for mesenchymal stromal cell (MSC) derived therapeutic efficacy

Ações bioquímicas/fisiológicas

FR180204 is a potent, cell-permeable, ATP-competitive inhibitor of ERK1 and ERK2 (mitogen-activated protein kinase (MAPK)/extracellular-signal-regulated kinases (ERK) 1/2).
FR180204 is a potent, selective, cell-permeable, ATP-competitive inhibitor of ERK1 and ERK2.
It can be used to study the roles of ERK as well as for drug development.

Características e benefícios

This compound is featured on the MAPKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

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


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Sigma-Aldrich

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Sigma-Aldrich

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Sigma-Aldrich

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Substrate stiffness and matrix composition coordinately control the differentiation of liver progenitor cells
Kourouklis AP, et al.
Biomaterials, 99, 82-94 (2016)
HOXB7 overexpression promotes cell proliferation and correlates with poor prognosis in gastric cancer patients by inducing expression of both AKT and MARKs
He X, et al.
Oncotarget, 8(1), 1247-1247 (2017)
Yuki Shindo et al.
Nature communications, 7, 10485-10485 (2016-01-21)
The phosphorylation cascade in the extracellular signal-regulated kinase (ERK) pathway is a versatile reaction network motif that can potentially act as a switch, oscillator or memory. Nevertheless, there is accumulating evidence that the phosphorylation response is mostly linear to extracellular
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Scientific reports, 8(1), 15726-15726 (2018-10-26)
The anti-proliferative activity of dietary flavonoid fisetin has been validated in various cancer models. Establishing its precise mechanism of action has proved somewhat challenging given the multiplicity of its targets. We demonstrated that YB-1 promotes epithelial-to-mesenchymal transition and its inhibition
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Cytokines of the transforming growth factor β (TGF-β) superfamily exert effects on proliferation, apoptosis and differentiation in various cell types. Cancer cells frequently acquire resistance to the anti-proliferative signals of TGF-β, which can be due to mutations in proteins of

Artigos

The mitogen-activated protein kinase (MAPK) family consists of both stress activated (SAPK) and mitogen-activated (MAPK) protein kinases. They form a network of signal transduction cascades that mediate cellular responses to a diverse range of stimuli, including growth factors, chemical or osmotic stress, irradiation, bacterial infection and proinflammatory cytokines.

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