Chemical Structure : SMARCA2 PROTAC YD23
CAS No.: 2951015-29-3
Catalog No.: PC-23133Not For Human Use, Lab Use Only.
SMARCA2 PROTAC YD23 is a potent and selective proteolysis targeting chimera (PROTAC) targeting SMARCA2 with DC50 of 64 nM in H1792 cells and Dmax of 88%.
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SMARCA2 PROTAC YD23 is a potent and selective proteolysis targeting chimera (PROTAC) targeting SMARCA2 with DC50 of 64 nM in H1792 cells and Dmax of 88%.
YD23 selectively degrades SMARCA2 and inhibits the growth of SMARCA4-mutant lung cancer cell lines.
YD23 exhibits DC50 of 297 nM and a Dmax of 95% in H1975 SMARCA4-WT cells, minimal impact on SMARCA4 up to 10 μM.
YD23 potently degraded SMARCA2 with a median DC50 of 92.8 nM and achieving a Dmax of 90% on an additional panel of ten SMARCA4-WT cell lines.
YD23 selectively inhibits growth of SMARCA4-mutant lung cancer cell lines with IC50 of 0.11 uM (SMARCA4-WT cells, IC50=6 uM).
SMARCA2 degradation disrupts chromatin accessibility at enhancers to disable cell cycle transcriptional programs.
YD23 (12.5 mg/kg) inhibits growth of SMARCA4-mutant xenograft models of lung cancer.
M.Wt | 738.78 | |
Formula | C38H39FN8O7 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-((2-(2-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-fluorophenoxy)ethoxy)ethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione |
1. Kotagiri S, et al. Cell Chem Biol. 2024 Oct 1:S2451-9456(24)00396-9.
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