Catalog No.: PC-26498Not For Human Use, Lab Use Only.
Cyclin D1 degrader MS28 (XY028-133) is a potent, selective and first-in-class PROTAC degrader of cyclin D1 through recruiting the CDK4/6-cyclin D1 complex to VHL E3 ligase, effectively degrades cyclin D1 in Calu-1 cells with DC50 of 950 nM and Dmax of 90% (8 h).
Cyclin D1 degrader MS28 (XY028-133) is a potent, selective and first-in-class PROTAC degrader of cyclin D1 through recruiting the CDK4/6-cyclin D1 complex to VHL E3 ligase, effectively degrades cyclin D1 in Calu-1 cells with DC50 of 950 nM and Dmax of 90% (8 h). MS28 displays modest degradation effects on CDK4/6 with DC50 > 10 μM and Dmax < 50% at the 8 h time point。 MS28 at 0.3 μM reduces the CDK6 protein level close to 50%, while it has no effect on CDK4. MS28 preferentially degrades Cyclin D1 over CDK4/6. MS28 degrades cyclin D1 by recruiting the CDK6-cyclin D1 complex to VHL, degrades cyclin D1 in a VHL-, CDK6- and UPS-dependent manner. MS28 does not degrade cyclin D2 or other major cyclins and CDKs, such as cyclin B1 and CDK2. MS28 effectively suppressed the proliferation of Calu-1 cells with GI50 of 1.0 uM, significantly reduced the mRNA levels of E2F target genes at 8 h of treatment in Calu-1 cells. MS28 phenocopied the effect of CCND1 KO in Calu-1 cells, inhibited the clonogenicity of Calu-1 cells.
