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Chemical Structure : MS3227
Catalog No.: PC-49672Not For Human Use, Lab Use Only.
MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.
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MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.
In WT TP53 leukemia cell lines, MS3227 led to activation of p53 targets p21, PUMA, and MDM2 and resulted in cell-cycle arrest, apoptosis, and decreased viability.
MS3227 also shows potent effect in primary patient specimens with selectivity towards leukemic blasts.
MS3227 enhanced the activity of other anti-leukemic agents including azacytidine, cytarabine, and venetoclax.
MS3227 treatment was shown to downregulate MCL-1, a known mediator of resistance to venetoclax.
| M.Wt | 1221.41 | |
| Formula | C62H83Cl2N7O10S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bridget K Marcellino, et al. Leukemia. 2022 Oct 29. doi: 10.1038/s41375-022-01735-6.
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