GSK1324726A
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.
GSK1324726A是BET蛋白的选择性小分子抑制剂,对BRD2、BRD3和BRD4的IC50值分别为41 nM、31 nM和22 nM[1]。
GSK1324726A与组蛋白H4多肽竞争性结合BET蛋白的溴区结构。它明显地抑制神经母细胞瘤株系中细胞生长(GI50值75 nM)。GSK1324726A也可以促进NET细胞死亡,其机制是GSK1324726A可以诱发这些细胞株的细胞毒性。GSK1324726A处理导致SK–N-AS、SK-N-SH和CHP-212细胞系在G1期被捕获。同时,在SK-N-SH和CHP-212细胞系中观察到Caspase 3/7的产生。在神经母细胞瘤增殖的小鼠中,GSK1324726A也显示了抑制肿瘤生长的能力[1]。
参考文献:
[1] Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.
Storage | Store at -20°C |
M.Wt | 434.91 |
Cas No. | 1300031-52-0 |
Formula | C25H23ClN2O3 |
Solubility | insoluble in H2O; ≥1.87 mg/mL in EtOH with gentle warming and ultrasonic; ≥17.7 mg/mL in DMSO |
SDF | Download SDF |
Canonical SMILES | OC(C(C=C1)=CC=C1C2=CC3=C(C=C2)N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)=O |
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。 |
描述 | GSK1324726A是BET蛋白的选择性小分子抑制剂,对BRD2、BRD3和BRD4的IC50值分别为41 nM、31 nM和22 nM。 | |||||
靶点 | BRD2 | BRD3 | BRD4 | |||
IC50 | 41 nM | 31 nM | 22 nM |
质量控制和MSDS
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