|
| | 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 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1364488-67-4.mol |  |
| | 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) |
| | 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-EE Preparation Products And Raw materials |
|
