ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine

K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine

Product NameK-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine
CAS191089-60-8
MFC33H48N2O6
MW568.76
EINECS
MOL File191089-60-8.mol

Chemical Properties

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
InChIKey	JXXCDAKRSXICGM-AOEKMSOUSA-N
SMILES	C1CCN(CCC/C=C/C2C=C(OC)C(OC)=C(OC)C=2)CCN1CCC/C=C/C1C=C(OC)C(OC)=C(OC)C=1

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

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 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 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.

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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