K-7174
K-7174
CAS: 191089-59-5
Molecular Formula: C33H48N2O6
K-7174 - Names and Identifiers
| Name | K-7174 |
| Synonyms | K7174 K-7174 K 7174 K-7174(FREE BASE) 1H-1,4-Diazepine, hexahydro-1,4-bis[(4E)-5-(3,4,5-trimethoxyphenyl)-4-penten-1-yl]- |
| CAS | 191089-59-5 |
K-7174 - Physico-chemical Properties
| Molecular Formula | C33H48N2O6 |
| Molar Mass | 568.74 |
| Solubility | Soluble in DMSO |
| Storage Condition | 2-8°C |
| Use | K-7174 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 inhibitor in 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 . 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. 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. 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 . |
K-7174 - Reference
| Reference Show more | 1: Fujiwara T, Ikeda T, Nagasaka Y, Okitsu Y, Katsuoka Y, Fukuhara N, Onishi Y, Ishizawa K, Ichinohasama R, Tomosugi N, Harigae H. A low-molecular-weight compound K7174 represses hepcidin: possible therapeutic strategy against anemia of chronic disease. PLoS One. 2013 Sep 27;8(9):e75568. doi: 10.1371/journal.pone.0075568. eCollection 2013. PubMed PMID: 24086573; PubMed Central PMCID: PMC3785497. 2: Kikuchi J, Yamada S, Koyama D, Wada T, Nobuyoshi M, Izumi T, Akutsu M, Kano Y, Furukawa Y. 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. doi: 10.1074/jbc.M113.480574. Epub 2013 Jul 22. PubMed PMID: 23878197; PubMed Central PMCID: PMC3757220. 3: Kikuchi J, Shibayama N, Yamada S, Wada T, Nobuyoshi M, Izumi T, Akutsu M, Kano Y, Sugiyama K, Ohki M, Park SY, Furukawa Y. Homopiperazine derivatives as a novel class of proteasome inhibitors with a unique mode of proteasome binding. PLoS One. 2013 Apr 11;8(4):e60649. doi: 10.1371/journal.pone.0060649. Print 2013. PubMed PMID: 23593271; PubMed Central PMCID: PMC3623906. 4: Shimada T, Hiramatsu N, Okamura M, Hayakawa K, Kasai A, Yao J, Kitamura M. Unexpected blockade of adipocyte differentiation by K-717 4: implication for endoplasmic reticulum stress. Biochem Biophys Res Commun. 2007 Nov 16;363(2):355-60. Epub 2007 Sep 6. PubMed PMID: 17869220. |
K-7174 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.758 ml | 8.791 ml | 17.583 ml |
| 5 mM | 0.352 ml | 1.758 ml | 3.517 ml |
| 10 mM | 0.176 ml | 0.879 ml | 1.758 ml |
| 5 mM | 0.035 ml | 0.176 ml | 0.352 ml |
Last Update：2024-01-02 23:10:35
K-7174 - Reference Information
| biological activity | K-7174 is a cell adhesion inhibitor, which can inhibit the expression of VCAM-1. |
Last Update：2024-04-10 22:29:15
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