SGC 0946
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SGC 0946是一种有效的蛋白甲基转移酶(PMT)DOT1L[一种特有的催化组蛋白H3赖氨酸79(H3K79)甲基化的赖氨酸甲基转移酶(PKMT)]小分子抑制剂,半数最大抑制浓度IC50值为0.3 nM[1]。
作为EPZ004777的溴化类似物,SGC 0946的细胞抑制能力比其前体有大幅提高,SGC 0946可在MCF10A(IC50:8.8 nM)和A431(IC50:2.65 nM)细胞中抑制H3K79的甲基化,相比之下EPZ004777的IC50分别为84 nM和264 nM。SGC 0946具有大幅增加的细胞抑制能力可归因于其更低的解离速率和更高的细胞透过性[1]。
参考文献:
[1] Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 618.57 |
Cas No. | 1561178-17-3 |
Formula | C28H40BrN7O4 |
Solubility | ≥30.95 mg/mL in DMSO; insoluble in H2O; ≥97.6 mg/mL in EtOH with ultrasonic |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C1=CC=C(NC(NCCCN(C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C4=NC=NC(N)=C4C(Br)=C3)O2)C(C)C)=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
Molm13白血病细胞以及A431细胞 |
溶解方法 |
在DMSO中的溶解度> 31 mg/ml。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
0-10 μM |
应用 |
在含有MLL/AF9易位的Molm13白血病细胞中,SGC0946能够时间以及浓度依赖性地降低H3K79me2水平。通过自动荧光显微镜定量分析MCF10A细胞中H3K79me2水平,研究发现与EPZ004777((IC50 84±20 nM)相比,SGC0946(IC50 8.8±1.6 nM)能够极大提高对DOT1L的抑制作用。相似的现象也在A431细胞系中观察到,SGC0946 和 EPZ004777的IC50值分别为2.65 nM 和264 nM。 |
References: [1] Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. |
Description | SGC 0946是一种有效的DOT1L甲基转移酶抑制剂,IC50值为0.3 nM。 | |||||
靶点 | DOT1L | |||||
IC50 | 0.3 nM |
质量控制和MSDS
- 批次: