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Merck

SML0320

FR180204

≥98% (HPLC), ERK1 and ERK2 inhibitor, powder

Synonyme(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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A propos de cet article

Formule empirique (notation de Hill) :
C18H13N7
Numéro CAS:
865362-74-9
Poids moléculaire :
327.34
UNSPSC Code:
12352200
PubChem Substance ID:
329825325
NACRES:
NA.77
MDL number:
MFCD14585805
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

Principaux documents

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Nom du produit

FR180204, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

faintly yellow to dark yellow

solubility

DMSO: ≥10 mg/mL

storage temp.

2-8°C

SMILES string

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)

InChI key

XVECMUKVOMUNLE-UHFFFAOYSA-N

Catégories apparentées

Application

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

Biochem/physiol Actions

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.

Features and Benefits

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000391910
0000391911
0000302342
0000302342
0000391911

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Consulter la Bibliothèque de documents

Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex
Ohori M, et al.
Biochemical and biophysical research communications, 336(1), 357-363 (2005)
The TLR4-PAR1 Axis Regulates Bone Marrow Mesenchymal Stromal Cell Survival and Therapeutic Capacity in Experimental Bacterial Pneumonia
Gupta N, et al.
Stem Cells, 36(5), 796-806 (2018)
Miho Tanaka et al.
Cancer research, 78(13), 3589-3603 (2018-04-25)
Natural killer (NK) cells express receptors specific for MHC class I (MHC-I) molecules involved in "missing-self" recognition of cancer and virus-infected cells. Here we elucidate the role of MHC-I-independent NKR-P1B:Clr-b interactions in the detection of oncogenic transformation by NK cells.
Mario Sechi et al.
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
Maren Bakkebø et al.
BMC immunology, 11, 57-57 (2010-11-26)
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
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