Product Data SheetK-7174Cat. No.:CAS No.:Molecular Formula:Molecular Weight:Target:Pathway:Storage:HY-12743191089-59-5C₃₃H₄₈N₂O₆568.74OthersOthersPlease store the product under the recommended conditions in the COA.Inhibitors•Agonists•Screening LibrariesSolvent & SolubilityIn Vitro10 mM in DMSOMass1 mg5 mg10 mgSolventConcentrationPreparing Stock Solutions1 mM5 mM10 mM1.7583 mL0.3517 mL0.1758 mL8.7914 mL1.7583 mL0.8791 mL17.5827 mL3.5165 mL1.7583 mLPlease refer to the solubility information to select the appropriate solvent.BIOLOGICAL ACTIVITYDescriptionK-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 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].1www.MedChemExpress.com
REFERENCES
[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.
[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.[3]. Shimada T, et al. Unexpected blockade of adipocyte differentiation by K-7174: implication for endoplasmic reticulum stress. Biochem Biophys Res Commun. 2007 Nov 16;363(2):355-60.
[4]. 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.
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