UNC0642
{[allProObj[0].p_purity_real_show]}
货号：A464128
UNC0642是一种对赖氨酸甲基转移酶G9a和GLP具有强效和选择性抑制作用的抑制剂，对G9a的IC50 小于2.5 nM。
UNC0642 化学结构
UNC0642 3D分子结构
规格
价格
会员价
库存
数量
{[ item.pr_size ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}
{[ getRatePrice(item.pr_rmb_sale, 1,1) ]}
{[ suihuo_tips(item.pr_tag_price) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}
{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]}
{[ suihuo_tips(item.pr_tag_price) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price) ]}
{[ getRatePrice(item.pr_rmb_sale, 1,1) ]}
{[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]}
{[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]}
现货
咨询
-
+
UNC0642 纯度/质量文件 产品仅供科研
货号：A464128
标准纯度：
{[allProObj[0].p_purity_real_show]}
产品说明书
全球学术期刊中引用的产品
• JMC , 2024. Ambeed. A918471 ,
A995972
]
• Anal. Chem. , 2024, 96(50): 19947-19954. Ambeed. A261947 ,
A1165388
]
• ACS Biomater. Sci. Eng. , 2024. Ambeed. A220462
]
• ACS Biomater. Sci. Eng. , 2024. Ambeed. A165235 ,
A110205
]
• Pharmaceutics , 2024, 16(12): 1546. Ambeed. A272538 ,
A187261 ,
A691302 ,
A506702
]
更多 >
UNC0642 质控信息
BRD4770
✔
99%+
UNC1999
+++
EZH2, IC50: 2 nM
EZH1, IC50: 45 nM
99%+
EPZ005687
++
98+%
EPZ015666
+++
99%+
3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
99%+
Tazemetostat
+++
EZH2, IC50: 11 nM
EZH2, Ki: 2.5 nM
98%
GSK126
++
99%+
MI-3
+
98%
MM-102
++
99%
EI1
++
EZH2 (Y641F), IC50: 13 nM
Ezh2 (wild-type), IC50: 15 nM
99% (HPLC)
SGC0946
++++
99%+
PFI-2 HCl
++++
SETD7, Ki: 0.33 nM
SETD7, IC50: 2 nM
99%+
Pinometostat
++++
99%+
EPZ004777
+++
99%+
Entacapone
++
95%
UNC0379
+
99%+
Menin-MLL inhibitor MI-2
+
98%
GSK343
+++
EZH2, IC50: 4 nM
EZH1, IC50: 240 nM
99%+
BIX-01294 3HCl
+
99%+
展开
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。
UNC0642 生物活性
描述
UNC0642 is the first G9a and GLP in vivo chemical probe with Ki value of 3.7nM, and displayed high in vitro potency for GLP with IC50<2.5nM. UNC0642 potently inhibited cellular inhibition of H3K9me2 with IC50 values of 110, 130, 130 and 40nM in MDA-MB-231, U2OS, PC3 and PANC-1 cell lines. UNC0642 reduced clonogenicity in PANC-1 cells in a concentration-dependent manner, at concentration of 0.5μM and 1μM, post 2 weeks, while it had no effect on clonogenicity in MDA-MB-231 cells[4] Snrpn to Ube3a (m+ /p∆S−U ) [5]
作用机制
UNC0642 is competitive with the substrate and non-competitive with the cofactor SAM.[4]
UNC0642 动物研究
Dose
Mice: 1 mg/kg - 4 mg/kg[3] [2]
Administration
i.p.
Pharmacokinetics
Animal
Mice[1]
Dose
5 mg/kg
Administration
i.p.
Cmax
947 ng/ml
Brain: plasma
0.33
AUC0→24h
1265 h·ng/ml
UNC0642 参考文献
[1] Liu F, Barsyte-Lovejoy D, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42.
[2] Kim Y, Lee HM, et al. Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat Med. 2017 Feb;23(2):213-222.
[3] Wang DY, Kosowan J, et al. Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice. Acta Pharmacol Sin. 2018 May;39(5):866-874.
[4] Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31. PMID: 24102134; PMCID: PMC3880643.
[5] Kim Y, Lee HM, Xiong Y, Sciaky N, Hulbert SW, Cao X, Everitt JI, Jin J, Roth BL, Jiang YH. Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat Med. 2017 Feb;23(2):213-222. doi: 10.1038/nm.4257. Epub 2016 Dec 26. PMID: 28024084; PMCID: PMC5589073.
展开
UNC0642 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.83mL
0.37mL
0.18mL
9.15mL
1.83mL
0.91mL
18.29mL
3.66mL
1.83mL
UNC0642 技术信息
搜索
