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YH 239-EE

Names

[ CAS No. ]:
1364488-67-4

[ Name ]:
YH 239-EE

[Synonym ]:
Ethyl 6-chloro-3-{1-[(4-chlorobenzyl)(formyl)amino]-2-[(2-methyl-2-propanyl)amino]-2-oxoethyl}-1H-indole-2-carboxylate
1H-Indole-2-carboxylic acid, 6-chloro-3-[1-[[(4-chlorophenyl)methyl]formylamino]-2-[(1,1-dimethylethyl)amino]-2-oxoethyl]-, ethyl ester
YH239-EE

Biological Activity

[Description]:

YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agentIC50 value:Target: MDM2/p53YH239-EE inhibits the growth of OCI-AML-3 cells with wild type p53 by inhibiting the p53-MDM2 interaction. YH239-EE induces cell cycle arrest and causes potent cell apoptosis via activation of p53 and downstream targets in four AML cells (OCI-AML-3 and MOLM-13 with wt p53, NB4 with p53 mutation, and HL60 with p53 deletion).

[Related Catalog]:

Signaling Pathways >> Apoptosis >> MDM-2/p53
Research Areas >> Cancer

[References]

[1]. Huang Y, et al. Discovery of highly potent p53-MDM2 antagonists and structural basis for anti-acute myeloid leukemia activities. ACS Chem Biol. 2014 Mar 21;9(3):802-11.


[Related Small Molecules]

Pifithrin-α hydrobromide | RG7388 | Nutlin-3a | AMG232 | Pifithrin-β (hydrobromide) | Stylomycin aminonucleoside | RG7112 | APR-246 | NVP-HDM201 | SAR 405838 | RITA (NSC 652287) | NVP-CGM097 | Tenovin-1 | SJ 172550

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
763.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H27Cl2N3O4

[ Molecular Weight ]:
504.406

[ Flash Point ]:
415.4±32.9 °C

[ Exact Mass ]:
503.137848

[ PSA ]:
91.50000

[ LogP ]:
4.85

[ Vapour Pressure ]:
0.0±2.6 mmHg at 25°C

[ Index of Refraction ]:
1.615

[ Storage condition ]:
-20℃

Related Compounds