2136247-12-4
2136247-12-4 structure
- Name: MD-224
- Chemical Name: MD-224
- CAS Number: 2136247-12-4
- Molecular Formula: C48H43Cl2FN6O6
- Molecular Weight: 889.80
- Catalog: Signaling Pathways Apoptosis MDM-2/p53
- Create Date: 2019-10-08 12:40:13
- Modify Date: 2024-01-15 18:44:20
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MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1].
| Name | MD-224 |
|---|
| Description | MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1]. |
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| Related Catalog | |
| In Vitro | MD-224 (1-30 nM; 2 hours) effectively induces depletion of MDM2 protein and concurrently accumulation of p53 protein in a dose-dependent manner in RS4;11 cells[1]. MD-224 (30 nM; 6 hours) is more potent than MI-1061 in induction of transcriptional upregulation of these p53 target genes but have no effect on TP53 itself in RS4;11 cells[1]. MD-224 (0.001-1 μM; 24hours) induces robust apoptosis at ≤10 nM in a dose-dependent manner upon a 24 hours treatment[1]. Western Blot Analysis[1] Cell Line: RS4;11 cells Concentration: 1 nM; 3 nM; 10 nM; 30 nM Incubation Time: 2 hours Result: Decreased MDM2 protein and accumulated of p53 protein. RT-PCR[1] Cell Line: RS4;11 cells Concentration: 30 nM Incubation Time: 6 hours Result: Upregulated p53 target gene expression. Apoptosis Analysis[1] Cell Line: RS4;11 cells Concentration: 0.001 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM Incubation Time: 24 hours Result: Induces robust apoptosis in RS4;11 cells. |
| References |
| Molecular Formula | C48H43Cl2FN6O6 |
|---|---|
| Molecular Weight | 889.80 |