MD-222

MD-222 is the first-in-class highly potent PROTAC degrader of MDM2 . MD-222 consists of ligands for Cereblon and MDM2 . MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects In Vitro MD-222 (1-30 nM; 1-2 hours) treatment shows very effective in reducing the levels of MDM2 protein and increasing the levels of p53 in a time- and dose-dependent manner in RS4;11 and RS4;11/IRMI-2 cells. MD-222 (30-100 nM; 6 hours) is effective in increasing the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA in RS4;11 cells, indicating strong activation of p53. MD-222 (4 days) shows cell growth inhibitory activity in RS4;11 cells with an IC50 of 5.5 nM, and has no effect on RS4;11/IRMI-2, MDA-MB-231 and MDA-MB-468 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: RS4;11 and RS4;11/IRMI-2 cells Concentration: 1 nM, 3 nM, 10 nM, 30 nM Incubation Time: 1 hour, 2 hours Result: Reduced the level of MDM2 and increased the level of p53. RT-PCRCell Line: RS4;11 cells Concentration: 30 nM, 100 nM Incubation Time: 6 hours Result: Increasd the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA. Form:Solid IC50& Target:MDM2

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet