货号	规格	价格	上海	北京	珠海	重庆	武汉
S87491-5mg	≥98%	￥1200.00 S87491-5mg ￥1200.00 3-5天	0 货期：3-5天	-	-	-	-
S87491-10mg	≥98%	￥1950.00 S87491-10mg ￥1950.00 3-5天	0 货期：3-5天	-	-	-	-
S87491-50mg	≥98%	￥6500.00 S87491-50mg ￥6500.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM

靶点：

IKK2:30 nM (IC50)

体外研究：

LY2409881 is an IKK2 inhibitor that inhibits TNFα-induced activation of NF-κB. By in vitro kinase assay, LY2409881 potently inhibits IKK2, with an IC50 of 30 nM. In contrast, the IC50 for IKK1 and other common kinases is at least one log higher. The specificity of LY2409881 for NF-κB signaling is further studied in a cell-based assay, by examining the effect of LY2409881 in the TNFα-dependent antiapoptosis function. TNFα is a well-characterized upstream stimulus of NF-κB. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity, whereas TNFα at 10 ng/mL does not cause any cytotoxicity. In contrast, coadministration of LY2409881 and TNFα results in markedly higher cell killing compared with LY2409881. This is because TNFα-dependent activation of antiapoptotic signals mediated by NF-κB is blocked by LY2409881, while the proapoptotic TNF receptor-associated death domain (TRADD) and FAS-associated death domain (FADD) cascade pathways activated by TNFα are not affected by LY2409881

体内研究：

A well-established xenograft model of DLBCL is used to confirm the activity of LY2409881 in vivo. SCID-beige mice implanted with LY10 cell-derived tumors are given intraperitoneal injections of LY2409881 twice weekly at three different doses: 50, 100, and 200 mg/kg. The treatments are well tolerated, resulting in no death or severe morbidity of the mice. The average tumor volume is graphed as a function of time for each treatment group. The rates of tumor volume growth of the treatment groups are all significantly slower than the untreated control group (P≤0.01)

参考文献：

1. Deng C, et al. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. Clin Cancer Res. 2015 Jan 1;21(1):134-45.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.062 ml	10.308 ml	20.617 ml
5 mM	0.412 ml	2.062 ml	4.123 ml
10 mM	0.206 ml	1.031 ml	2.062 ml
50 mM	0.041 ml	0.206 ml	0.412 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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