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.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
YH239-EE is a potent antagonist of p53-MDM2 .
p53 is a transcription factor and functions as a tumor suppressor. MDM2 is a negative regulator of p53. The interaction of p53 and MDM2 has emerged as a novel target for anticancer drugs .
YH239-EE is a potent p53-MDM2 antagonist. In OCI-AML-3 cells, YH239-EE potently inhibited cell proliferation. In AML cell lines, YH239-EE induced a cell cycle arrest and cell accumulation in the sub-G1 phase. YH239-EE induced apoptosis by 11.8-fold, 5.6-fold and 13.1-fold in OCI-AML-3, MOLM-13 and NB4 AML cell lines, respectively. In MOLM-13 cells, YH239 exhibited almost no apoptotic effect. However, YH239-EE significantly induced apoptosis. In MOLM-13 cells, (+)-YH239-EE and (−)-YH239-EE inhibited metabolic activity with EC50 values of 7.5 μM and 25.2 μM and induced apoptosis with 13.7% and 51.5% viable cells, respectively. (+)-YH239-EE (20 μM) induced p53 and significantly activated caspase 3 and 7 .
. 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|
|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|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|
|Description||YH239-EE is a potent antagonist of p53-MDM2 and an inducer of apoptosis.|