YH239-EE
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.
YH239-EE是一种有效的p53-MDM2拮抗剂[1].
p53是一种转录因子,是一种肿瘤抑制子.MDM2是p53的负调控子.p53和MDM2的相互作用是新的抗癌药物靶点[1].
YH239-EE是一种有效的p53-MDM2拮抗剂.在OCI-AML-3细胞中,YH239-EE可有效抑制细胞增殖.在AML细胞系中,YH239-EE可诱发细胞周期停滞以及亚G1期细胞积累.YH239-EE可分别在OCI-AML-3\MOLM-13和NB4 AML细胞系中诱导11.8倍\5.6倍和13.1倍的细胞凋亡.在MOLM-13细胞中,YH239几乎没有凋亡效应.但是,YH239-EE可显著诱发细胞凋亡.在MOLM-13细胞中.(+)-YH239-EE和()-YH239-EE可抑制代谢活性,EC50值分别为7.5 μM和25.2 μM,分别诱导13.7%和51.5%的活细胞凋亡.(+)-YH239-EE(20 μM)可诱导p53,并能显著激活caspase 3和7[1].
参考文献:
[1]. Huang Y, Wolf S, Beck B, et al. Discovery of highly potent p53-MDM2 antagonists and structural basis for anti-acute myeloid leukemia activities. ACS Chem Biol, 2014, 9(3): 802-811.
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 504.41 |
Cas No. | 1364488-67-4 |
Formula | C25H27Cl2N3O4 |
Solubility | ≥50.4 mg/mL in DMSO; insoluble in H2O; ≥4.26 mg/mL in EtOH with ultrasonic |
Chemical Name | (Z)-N-(tert-butyl)-2-(6-chloro-2-(ethoxycarbonyl)-1H-indol-3-yl)-2-(N-(4-chlorobenzyl)formamido)acetimidic acid |
SDF | Download SDF |
Canonical SMILES | CCOC(C1=C(C(N(C=O)CC2=CC=C(Cl)C=C2)/C(O)=N/C(C)(C)C)C3=C(N1)C=C(Cl)C=C3)=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。 |
Description | YH239-EE是一种有效的p53-MDM2拮抗剂和细胞凋亡诱导剂. | |||||
靶点 | p53-MDM2 | |||||
IC50 |
质量控制和MSDS
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