貨號	規格	價格	上海	北京	武漢	南京
S83988-5mg	99.5%	￥765.00 S83988-5mg ￥765.00 現貨	6 6	-	-	-
S83988-10mg	99.5%	￥1105.00 S83988-10mg ￥1105.00 現貨	7 7	-	-	-
S83988-25mg	99.5%	￥1615.00 S83988-25mg ￥1615.00 現貨	6 6	-	-	-
S83988-50mg	≥99%	￥2975.00 S83988-50mg ￥2975.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

產品描述：

NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

靶點：

IC50: 5 nM (PAK1);PAK

體外研究：

NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved

體內研究：

NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)

參考文獻：

1. Karpov AS, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.084 ml	10.418 ml	20.837 ml
5 mM	0.417 ml	2.084 ml	4.167 ml
10 mM	0.208 ml	1.042 ml	2.084 ml
50 mM	0.042 ml	0.208 ml	0.417 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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