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YH239-EE

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YH239-EE Basic information

Product Name:
YH239-EE
Synonyms:
  • Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-carboxylate
  • YH239-EE ethyl 3-[2-(tert-butylamino)-1-[(4-chlorophenyl)methyl-formylamino]-2-oxoethyl]-6-chloro-1H-indole-2-carboxylate
  • Ethyl 3-[2-(tert-Butylamino)-1-[N-(4-chlorobenzyl)formamido]-2-oxoet
  • YH239-EE 6-Chloro-3-[1-[[(4-chlorophenyl)methyl]formylamino]-2-[(1,1-dimethylethyl)amino]-2-oxoethyl]-1H-indole-2-carboxylic acid Ethyl Ester
  • ethyl 3-[2-(tert-butylamino)-1-[(4-chlorophenyl)methyl-formylamino]-2-oxoethyl]-6-chloro-1H-indole-2-carboxylate
  • Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-
  • YH239-EE
  • YH 239-EE;YH 239 EE
CAS:
1364488-67-4
MF:
C25H27Cl2N3O4
MW:
504.41
Product Categories:
  • Inhibitors
Mol File:
1364488-67-4.mol
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YH239-EE Chemical Properties

Boiling point:
763.3±60.0 °C(Predicted)
Density 
1.313±0.06 g/cm3(Predicted)
storage temp. 
Desiccate at -20°C
solubility 
≥50.4 mg/mL in DMSO; insoluble in H2O; ≥4.26 mg/mL in EtOH with ultrasonic
form 
solid
pka
13.20±0.30(Predicted)
color 
White to off-white
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YH239-EE Usage And Synthesis

Uses

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

Biological Activity

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].

target

p53-MDM2

storage

Store at -20°C

References

[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.

YH239-EESupplier

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