貨號	規格	價格	上海	北京	武漢	南京
S83742-1mg	98.4%	￥520.00 S83742-1mg ￥520.00 現貨	9 9	-	-	-
S83742-5mg	98.4%	￥1610.00 S83742-5mg ￥1610.00 現貨	6 6	-	-	-
S83742-10mg	98.4%	￥2350.00 S83742-10mg ￥2350.00 現貨	6 6	-	-	-
S83742-25mg	98.4%	￥3850.00 S83742-25mg ￥3850.00 現貨	6 6	-	-	-

產品介紹

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

產品描述：

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

靶點：

IC50: 15.1 nM (KDM5); EC50: 0.34 μM (PC9 H3K4Me3);HistoneDemethylase

體外研究：

KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A

體內研究：

When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo

參考文獻：

1. Liang J, et al. Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.083 ml	15.414 ml	30.828 ml
5 mM	0.617 ml	3.083 ml	6.166 ml
10 mM	0.308 ml	1.541 ml	3.083 ml
50 mM	0.062 ml	0.308 ml	0.617 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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