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SGC0946 {[allProObj[0].p_purity_real_show]}

货号:A702574

SGC0946 is a selective inhibitor of DOT1L methyltransferase with IC50 of 0.3 nM and can kill mixed lineage leukaemia cells.

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SGC0946 化学结构 CAS号:1561178-17-3
SGC0946 化学结构
CAS号:1561178-17-3
SGC0946 3D分子结构
CAS号:1561178-17-3
SGC0946 化学结构 CAS号:1561178-17-3
SGC0946 3D分子结构 CAS号:1561178-17-3
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SGC0946 纯度/质量文件 产品仅供科研

货号:A702574 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 99%+
UNC1999 +++

EZH1, IC50: 45 nM

EZH2, IC50: 2 nM

99%+
EPZ005687 ++

EZH2, Ki: 24 nM

98+%
EPZ015666 +++

PRMT5, Ki: 5 nM

99%+
3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

99%+
Tazemetostat +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

98%
GSK126 ++

EZH2, IC50: 9.9 nM

99%+
MI-3 +

Menin-MLL, IC50: 648 nM

98%
MM-102 ++

MLL1, IC50: 0.4 μM

99%
EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

98%
SGC0946 ++++

DOT1L, IC50: 0.3 nM

99%+
PFI-2 HCl ++++

SETD7, Ki: 0.33 nM

SETD7, IC50: 2 nM

99%+
Pinometostat ++++

DOT1L, Ki: 80 pM

99%+
EPZ004777 +++

DOT1L, IC50: 0.4 nM

99%+
Entacapone ++

COMT, IC50: 151 nM

95%
UNC0379 +

SETD8, IC50: 7.9 μM

99%+
Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

98%
GSK343 +++

EZH1, IC50: 240 nM

EZH2, IC50: 4 nM

99%+
BIX-01294 3HCl +

G9a, IC50: 2.7 μM

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。

SGC0946 生物活性

靶点
  • Histone Methyltransferase

    DOT1L, IC50:0.3 nM

描述 SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibit potential of cell self-renewal and metastatic, and also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells[1].[2].[3].
体内研究

Administering SGC0946 at 10 mg/kg intraperitoneally twice weekly for six weeks notably hinders tumor growth in a mouse model of orthotopic xenograft ovarian cancer, while concurrently reducing DOT1L enzymatic action and the levels of H3K79me2, CDK6, and cyclin D3 within the tumors.

体外研究

SGC0946 demonstrates a capacity to inhibit DOT1L activity with an IC50 of 2.65 nM in A431 cells over a period of 4 days at concentrations ranging from 0 to 100 μM[1].

When administered at 1 and 5 μM for 14 days, SGC0946 selectively diminishes cell viability in a leukaemia model derived from human cord blood cells harboring the MLL-AF9 fusion gene[1].

At a concentration of 1 μM over 3 to 7 days, SGC0946 progressively diminishes the H3K79me2 mark in the Molm13 MLL cell line, which possesses the MLL/AF9 translocation[1].

With a 7-day treatment of 1 μM, SGC0946 effectively downregulates the expression of MLL target genes, namely HOXA9 and Meis1[1].

Through 12 days of treatment with SGC0946 at doses of 0.2, 2, or 20 μM, the proliferation and survival of ovarian cancer cells are curtailed by the inhibition of DOT1L's enzymatic function[2].

Employing 10 μM of SGC0946 for 12 days results in G1 phase arrest in SK-OV-3 and TOV21G cells by targeting DOT1L[2].

SGC0946 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human MCF10A cells Function assay Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level, IC50=0.0088 μM 25406853

SGC0946 动物研究

Dose Mice: 4 mg/kg[2] (i.p.), 10 mg/kg[3] (i.p.)
Administration i.p.

SGC0946 参考文献

[1]Yu W, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.

[2]Zhang X, et al. Prognostic and therapeutic value of disruptor of telomeric silencing-1-like (DOT1L) expression in patients with ovarian cancer. J Hematol Oncol. 2017 Jan 23;10(1):29.

[3]Zhang L, et al. Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Oncotarget. 2014 Nov 15;5(21):10665-77.

SGC0946 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.08mL

1.62mL

0.81mL

16.17mL

3.23mL

1.62mL

SGC0946 技术信息

CAS号1561178-17-3
分子式C28H40BrN7O4
分子量 618.566
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 50 mg/mL(80.83 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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