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MRT68921 hydrochloride {[allProObj[0].p_purity_real_show]}

货号:A695028 同义名: MRT68921 HCl

MRT68921 HCl is a selective inhibitor of ULK1 and ULK2 with IC50 0f 2.9 nM and 1.1 nM.

MRT68921 hydrochloride 化学结构 CAS号:2070014-87-6
MRT68921 hydrochloride 化学结构
CAS号:2070014-87-6
MRT68921 hydrochloride 3D分子结构
CAS号:2070014-87-6
MRT68921 hydrochloride 化学结构 CAS号:2070014-87-6
MRT68921 hydrochloride 3D分子结构 CAS号:2070014-87-6
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MRT68921 hydrochloride 纯度/质量文件 产品仅供科研

货号:A695028 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

97%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

97%
Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

MRT68921 hydrochloride 生物活性

靶点
  • Autophagy

    ULK1, IC50:2.9 nM

    ULK2, IC50:1.1 nM

描述 ULK1 (unc-51-like kinase 1), a serine/threonine protein kinase, is essential for the initial stages of autophagy and can be targeted to block autophagy for disease therapy[2]. MRT68921 hydrochloride is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nM) and greater than a 30-fold reduction for ULK2 (1.1 nM)[2]. In line with the in vitro IC50 values, 1 μM MRT68921 was sufficient to reduce phospho-ATG13 which was used as a measure of ULK1 activity to control levels. Therefore, this compound could reduce ULK1 activity in cells. Importantly, it also blocked autophagy as indicated by LC3-II levels[2].

MRT68921 hydrochloride 参考文献

[1]Petherick KJ, Conway OJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 Nov 27;290(48):28726.

[2]Petherick KJ, Conway OJ, Mpamhanga C, Osborne SA, Kamal A, Saxty B, Ganley IG. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. doi: 10.1074/jbc.C114.627778. Epub 2015 Apr 1. Erratum in: J Biol Chem. 2015 Nov 27;290(48):28726. PMID: 25833948; PMCID: PMC4416842.

MRT68921 hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.23mL

4.25mL

2.12mL

MRT68921 hydrochloride 技术信息

CAS号2070014-87-6
分子式C25H35ClN6O
分子量 471.038
别名 MRT68921 HCl
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度
动物实验配方
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