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Merck

SML3105

K-7174 dihydrochloride

≥98% (HPLC)

Sinónimos:

1,4-bis((E)-5-(3,4,5-Trimethoxyphenyl)pent-4-enyl)-1,4-diazepane dihydrochloride, K 7174 dihydrochloride, K7174 dihydrochloride, N,N?-bis-(E)-[5-(3,4,5-Trimethoxyphenyl)-4-pentenyl]homopiperazine dihydrochloride

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About This Item

Fórmula empírica (notación de Hill):
C33H48N2O6 · 2HCl
Número CAS:
191089-60-8
Peso molecular:
641.67
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD28900671

Nombre del producto

K-7174 dihydrochloride, ≥98% (HPLC)

InChI key

JKAQFPBRMVEHBD-CHBZAFCASA-N

SMILES string

COC(C(OC)=C1)=C(C=C1/C=C/CCCN(CCC2)CCN2CCC/C=C/C3=CC(OC)=C(C(OC)=C3)OC)OC.[H]Cl.[H]Cl

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

−20°C

Quality Level

100

Categorías relacionadas

Biochem/physiol Actions

K-7174 is a homopiperazine with dual GATA and proteasome inhibitory activtiy. K-7174 selective inhibts GATA-mediated gene regulations in cultures (10-30 μM; VCAM-1 expression in HUVECs or Epo suppression in Hep3B cells) and in vivo (30 mg/kg in mice via i.p. against IL-1beta- or TNF-alpha-induced anemia). K-7174 exhibits anti-myeloma activity in vitro (10-25 μM) and in vivo (50 mg/kg/day p.o. in mice) by targeting the active pockets of β1, β2 and β5 subunits of proteasome along hydrophobic grooves in the direction of the β7, β1 and β4 subunits in a manner distinct from that of bortezomib.
Orally active, dual GATA and proteasome inhibitor in vitro and in vivo.

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
0000130304
0000130305
0000127294

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Jiro Kikuchi et al.
The Journal of biological chemistry, 288(35), 25593-25602 (2013-07-24)
Bortezomib therapy is now indispensable for multiple myeloma, but is associated with patient inconvenience due to intravenous injection and emerging drug resistance. The development of orally active proteasome inhibitors with distinct mechanisms of action is therefore eagerly awaited. Previously, we
M Umetani et al.
Biochemical and biophysical research communications, 272(2), 370-374 (2000-06-02)
A novel inhibitor for the adhesion of monocytes to cytokine-stimulated endothelial cells, K-7174, was selected by an assay system using the cultured human monocytic cells and human endothelial cells. K-7174 inhibited the expression of vascular cell adhesion molecule-1 (VCAM-1) induced
Yosuke Takano et al.
Biochemical and biophysical research communications, 360(2), 470-475 (2007-07-03)
K-7174, a GATA-specific inhibitor, is a putative anti-inflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. However, molecular mechanisms involved have not been elucidated. We found that, in glomerular podocytes, induction of monocyte chemoattractant protein 1 (MCP-1)
Sergio Martinez-Høyer et al.
Nature cell biology, 22(5), 526-533 (2020-04-07)
Interstitial deletion of the long arm of chromosome 5 (del(5q)) is the most common structural genomic variant in myelodysplastic syndromes (MDS)1. Lenalidomide (LEN) is the treatment of choice for patients with del(5q) MDS, but half of the responding patients become
Shigehiko Imagawa et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 17(12), 1742-1744 (2003-09-06)
Interleukin-1beta (IL-1beta), tumor necrosis factor-alpha (TNF-alpha), or N(G)-monomethyl-L-arginine (L-NMMA) are increased in patients with chronic disease-related anemia. They increase the binding activity of GATA and inhibit erythropoietin (Epo) promoter activity. In this study, we examined the ability of K-7174 (a
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