K-7174 dihydrochloride

• CAT Number: I007475
• CAS Number: 191089-60-8
• Molecular Formula: C33H50Cl2N2O6
• Molecular Weight: 641.67
• Purity: ≥95%
• Synonyms: 1,4-bis[(E)-5-(3,4,5-trimethoxyphenyl)pent-4-enyl]-1,4-diazepane;dihydrochloride
• InChI: InChI=1S/C33H48N2O6.2ClH/c1-36-28-22-26(23-29(37-2)32(28)40-5)14-9-7-11-16-34-18-13-19-35(21-20-34)17-12-8-10-15-27-24-30(38-3)33(41-6)31(25-27)39-4;;/h9-10,14-15,22-25H,7-8,11-13,16-21H2,1-6H3;2*1H/b14-9+,15-10+
• InChIKey: JKAQFPBRMVEHBD-CHBZAFCASA-N
• SMILES: COC1=CC(=CC(=C1OC)OC)C=CCCCN2CCCN(CC2)CCCC=CC3=CC(=C(C(=C3)OC)OC)OC.Cl.Cl

K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer[1][2][3].
K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand[1].
K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM[1].
K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM[1].
K-7174 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells[2].
K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA[2].
K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis[3].
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].

Reference

[1]. Umetani M, et al. A novel cell adhesion inhibitor, K-7174, reduces the endothelial VCAM-1 induction by inflammatory cytokines, acting through the regulation of GATA. Biochem Biophys Res Commun. 2000 Jun 7;272(2):370-4.
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[2]. Imagawa S, et al. A GATA-specific inhibitor (K-7174) rescues anemia induced by IL-1beta, TNF-alpha, or L-NMMA. FASEB J. 2003 Sep;17(12):1742-4.
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[3]. Kikuchi J, et al. The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. J Biol Chem. 2013 Aug 30;288(35):25593-602.
 [Content Brief]