PROTAC NSD2 degrader-1
PROTAC NSD2 degrader-1 is a PROTAC degrader that selectively targets NSD2, with a DC50 of 0.37 μM. PROTAC NSD2 degrader-1 induces selective degradation of long and short isoforms of NSD2 containing the PWWP1 domain by forming a ternary complex with FBXO22. NSD2 degradation mediated by PROTAC NSD2 degrader-1 depends on the ubiquitin-proteasome system and the neddylation pathway. PROTAC NSD2 degrader-1 can be used in cancer-related research such as non-small cell lung cancer, multiple myeloma and prostate cancer.
(Pink: Target protein ligand; Blue: Ligands for E3 Ligase E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3108071-48-0
- Formula: C38H34N4O6
- Molecular Weight:642.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NSD2 0.37 μM (DC50) |
PROTAC NSD2 degrader-1 (compound T9) potently induces NSD2 degradation in HEK293T-NSD2-HiBiT cells, with a DC50 of 0.37 μM[1].
PROTAC NSD2 degrader-1 (2 μM; 10 μM MG132 (HY-13259), 1 μM MLN4924 (HY-70062); 4 h) mediates the degradation of NSD2 in H358 cells via the proteasome- and ubiquitin-like modification-dependent ubiquitin-proteasome system pathway[1].
PROTAC NSD2 degrader-1 (2 μM; 48 h siRNA treatment; 4 h incubation) induces NSD2 degradation in H358 cells, and this process is dependent on the E3 ligase FBXO22, as knockdown of FBXO22 partially restores NSD2 protein levels[1].
PROTAC NSD2 degrader-1 (2.5-5 μM; 4 h) induces NSD2 degradation in H358 cells, and this process is independent of amine oxidase activity, as its degradation efficiency is comparable in oxidase-free medium and complete medium[1].
PROTAC NSD2 degrader-1 (0.001-10 μM) dose-dependently promotes the formation of a ternary complex between NSD2 and FBXO22 in 293T cells, where covalent binding at the Cys326 site of FBXO22 is critical for optimal complex formation[1].
PROTAC NSD2 degrader-1 (2 μM; 4 h) induces degradation of NSD2 in 293T cells, a process that requires covalent binding to Cys326 of FBXO22, as the FBXO22C326A mutant blocks this degradation[1].
PROTAC NSD2 degrader-1 (0.1-10 μM; 4 h) induces dose-dependent degradation of both the long and short isoforms of NSD2 in H358 cells[1].
PROTAC NSD2 degrader-1 (2 μM; 2-8 h) induces rapid time-dependent degradation of both long and short isoforms of NSD2 in H358 cells[1].
PROTAC NSD2 degrader-1 (10 μM; 4 h) induces significant NSD2 degradation in PC3 cells[1].
PROTAC NSD2 degrader-1 (0.1-10 μM; 4 days) exerts dose-dependent inhibitory effects on the cell proliferation of PC3 and H358 cancer cells during the 4-day treatment[1].
PROTAC NSD2 degrader-1 (1-10 μM; 24 h) inhibits the migration of PC3 prostate cancer cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H358 nonsmall cell lung cancer cells
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Concentration:0.1, 1, 2, 10 μM
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Incubation Time:4 h
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Result:Induced dose-dependent degradation of both NSD2 long and short isoforms.
Achieved substantial reduction of both isoforms at 2 μM.
Induced over 50% degradation of total NSD2 at 1 μM.
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Cell Line:H358 nonsmall cell lung cancer cells
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Concentration:2 μM
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Incubation Time:2, 4, 6, 8 h
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Result:Induced substantial NSD2 degradation within 2 h, eliminating ~70% of protein.
Achieved maximal degradation by 4 h.
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Cell Line:PC3 prostate cancer cells
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Concentration:10 μM
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Incubation Time:4 h
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Result:Induced significant degradation of NSD2 at 10 μM.
No apparent degradation was observed with a comparator degrader at the same concentration.
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Cell Line:H358 nonsmall cell lung cancer cells
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Concentration:2 μM
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Incubation Time:48 h 10 nM siRNA treatment
4 h incubation -
Result:FBXO22 knockdown partially rescued NSD2 protein levels.
Scrambled siRNA had no effect on NSD2 protein levels.
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Cell Line:H358 nonsmall cell lung cancer cells
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Concentration:2.5, 5 μM
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Incubation Time:4 h
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Result:Maintained comparable NSD2 degradation efficiency in both oxidase-free Opti-MEM and complete RPMI1640+10%FBS media.
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Cell Line:FBXO22 knockout 293T cells
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Concentration:2 μM
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Incubation Time:4 h
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Result:Induced significant NSD2 degradation in cells transfected with wild-type FBXO22.
Failed to induce degradation in cells transfected with the FBXO22 C326A mutant or empty vector.
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Cell Line:PC3 prostate cancer cells
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Concentration:1, 5, 10 μM
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Incubation Time:24 h
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Result:Induced dose-dependent inhibition of cell migration.
Reduced migration to ~45% of control at 10 μM.
Reduced migration to ~60% of control at 5 μM.
Showed no significant difference from control at 1 μM.
Chemical Information
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CAS No. 3108071-48-0
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Molecular Weight 642.70
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Formula C38H34N4O6
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SMILES
O=C(N(C1CC1)CC2=CC=C(C(NC3=CC=C(CN(C(CC4=CC=C(C=O)C=C4)=O)CC5)C5=C3)=O)C=C2)C6=CC7=C(C=C6)NC(CO7)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC NSD2 degrader-1 Related Classifications
HY-184968 Related Classifications
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