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YH239-EE

Catalog No.
B4756
p53-MDM2 antagonist, potent
Grouped product items
SizePriceStock Qty
10mg
$88.00
In stock
50mg
$355.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

YH239-EE is a potent antagonist of p53-MDM2 [1].

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 [1].

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 [1].

Reference:
[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.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt504.41
Cas No.1364488-67-4
FormulaC25H27Cl2N3O4
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
SDFDownload SDF
Canonical SMILESCCOC(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
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor 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.

Biological Activity

Description YH239-EE is a potent antagonist of p53-MDM2 and an inducer of apoptosis.
Targets p53-MDM2          
IC50            

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