| Identification | Back Directory | [Name]
K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine | [CAS]
191089-60-8 | [Synonyms]
K-7174 2HCl
K-7174 dihydrochloride
K7174; K 7174; K-7174; K-7174-2HCL; K-7174 DIHYDROCHLORIDE.
1,4-Bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl)-1,4-diazepane
K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine | [Molecular Formula]
C33H48N2O6 | [MDL Number]
MFCD12922512 | [MOL File]
191089-60-8.mol | [Molecular Weight]
568.76 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Water:15.0(Max Conc. mg/mL);23.38(Max Conc. mM) | [form ]
A crystalline solid | [color ]
White to yellow | [Water Solubility ]
H2O: 2mg/mL, clear |
| Hazard Information | Back Directory | [Uses]
K-7174, a GATA-specific inhibitor, is a putative antiinflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. | [Biological Activity]
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 β1β2 and β5 subunits of proteasome along hydrophobic grooves in the direction of the β7β1 and β4 subunits in a manner distinct from th at of bortezomib. | [in vivo]
K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α[2].
K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo[3].
K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection[3]. | Animal Model: | ICR mice with IL-β or TNF-α injection[2] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection; 30 mg/kg once daily for 9 days | | Result: | Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations. |
| Animal Model: | NOD/SCID mice with murine xenograft[3] | | Dosage: | 75 mg/kg | | Administration: | Intraperitoneal injection; once daily for 14 days | | Result: | Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
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| Animal Model: | NOD/SCID mice with murine xenograft[3] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; once daily for 14 days | | Result: | Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.
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| [storage]
Store at -20°C |
|
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|