3033543-95-9
Chemical Structure
PROTAC NSD3 degrader-1
- CAS No.: 3033543-95-9
- Formula:C56H71FN8O4S
- Molecular Weight:971.28
InChIKey: BOTJARXURVIORK-NOXIQMFQSA-N
SMILES: CC1=C(C(C)=CC(CNCCCCCCCCCCC(N[C@H](C(N2[C@@H](C[C@H](C2)O)C(N[C@H](C3=CC=C(C=C3)C4=C(N=CS4)C)C)=O)=O)C(C)(C)C)=O)=C1)C5=C(N(C=N5)C)C6=CC=NC7=C6C=CC(F)=C7
Biological Activity: PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
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PROTAC NSD3 degrader-1 | 99.40% | PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP. | ||||||||||||||||||||
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Keywords
