WDR5-IN-1

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WDR5-IN-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2408842-51-1

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议

产品介绍

WDR5-IN-1 是一种有效的选择性 WD 重复结构域 5 (WDR5) 抑制剂，Kd 为<0.02 nM。WDR5-IN-1 抑制 MLL1 组蛋白甲基转移酶活性 (HMT)，IC50为 2.2 nM。WDR5-IN-1 减少 WDR5 移位基因的 MYC 募集，并在 CHP-134 (神经母细胞瘤) 和 Ramos (Burkitt淋巴瘤) 细胞系中显示出有效的抗增殖作用。

Cas No.	2408842-51-1
分子式	C₃₀H₃₁FN₄O₃
分子量	514.59
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of<0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1]. WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1].WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1].WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM[1]. [1]. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675.