YH239-EE
- CAS NO.:1364488-67-4
- Empirical Formula: C25H27Cl2N3O4
- Molecular Weight: 504.41
- MDL number: MFCD28099816
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:20
What is YH239-EE?
The Uses of YH239-EE
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].
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.
Properties of YH239-EE
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 |
Safety information for YH239-EE
Computed Descriptors for YH239-EE
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