K-7174 (dihydrochloride)
Names
[ CAS No. ]:
191089-60-8
[ Name ]:
K-7174 (dihydrochloride)
[Synonym ]:
1,4-Bis[(4E)-5-(3,4,5-trimethoxyphenyl)-4-penten-1-yl]-1,4-diazepane
1H-1,4-Diazepine, hexahydro-1,4-bis[(4E)-5-(3,4,5-trimethoxyphenyl)-4-penten-1-yl]-
K-7174 (dihydrochloride)
Biological Activity
[Description]:
K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.IC50 value:Target: GATA-specific inhibitorin vitro: K-7174 inhibited the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either tumor necrosis factor alpha or interleukin-1beta, without affecting the induction of intercellular adhesion molecule-1 or E-selectin. K-7174 had no effect on the stability of VCAM-1 mRNA.K-7174 did not influence the binding to any of the following binding motifs: octamer binding protein, AP-1, SP-1, ets, NFkappaB, or interferon regulatory factor [1]. Addition of 10 microM K-7174 rescued these inhibitions of Epo protein production and promoter activity induced by IL-1beta, TNF-alpha, or L-NMMA, respectively [2]. K-7174 had the potential to induce endoplasmic reticulum (ER) stress evidenced by induction of GRP78 and CHOP.Other inducers of ER stress completely reproduced the effects of K-7174 including suppression of lipid accumulation, blockade of induction of adiponection and PPARgamma and maintenance of MCP-1 expression [3].in vivo: K-7174, one of proteasome inhibitory homopiperazine derivatives, exhibits a therapeutic effect, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. Moreover, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [4].
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.1±0.1 g/cm3
[ Boiling Point ]:
689.9±55.0 °C at 760 mmHg
[ Molecular Formula ]:
C33H50Cl2N2O6
[ Molecular Weight ]:
641.67
[ Flash Point ]:
171.2±28.7 °C
[ LogP ]:
5.61
[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C
[ Index of Refraction ]:
1.552
[ Storage condition ]:
2-8℃