SGC0946

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Chemical Structure| 1561178-17-3 同义名 : -
CAS号 : 1561178-17-3
货号 : A702574
分子式 : C28H40BrN7O4
纯度 : 99%+
分子量 : 618.57
MDL号 : MFCD26523136
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
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
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
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
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.