貨號	規格	價格	上海	北京	武漢	南京
S84156-5mg	≥99%	￥880.00 S84156-5mg ￥880.00 2-3天	0 貨期：2-3天	-	-	-
S84156-10mg	≥99%	￥1500.00 S84156-10mg ￥1500.00 2-3天	0 貨期：2-3天	-	-	-
S84156-50mg	≥99%	￥6400.00 S84156-50mg ￥6400.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

靶點：

Proteasome;Apoptosis;mTOR

體外研究：

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. 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. K-7174 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells. K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA. K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis. Cell Viability Assay Cell Line: KMS12-BM, U266, and RPMI8226 cell lines Concentration: 0-25 μM Incubation Time: 72 h Result: Inhibited MM cells growth. Apoptosis Analysis Cell Line: KMS12-BM, U266, and RPMI8226 cell lines Concentration: 10 μM Incubation Time: 48 h Result: Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.

體內研究：

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. 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. Animal Model: ICR mice with IL-β or TNF-α injection 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 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 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.

參考文獻：

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. 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.

溶解性：

Soluble in H2O

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.558 ml	7.792 ml	15.584 ml
5 mM	0.312 ml	1.558 ml	3.117 ml
10 mM	0.156 ml	0.779 ml	1.558 ml
50 mM	0.031 ml	0.156 ml	0.312 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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K-7174 (dihydrochloride)