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Art. -Nr.: HY-184968

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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).

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CAS. Nr.: 3108071-48-0
Formel: C₃₈H₃₄N₄O₆
Molecular Weight:642.70

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC NSD2 degrader-1 Chemical Structure

CAS. Nr.: 3108071-48-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: Target protein ligand; Blue: Ligands for E3 Ligase E3 ligase ligand; Black: linker).

IC₅₀ & Target^[1]

NSD2

0.37 μM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

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 FBXO22^C326A 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.

Western Blot Analysis^[1]

Cell Line:

H358 nonsmall cell lung cancer cells
Concentration:

0.1, 1, 2, 10 μM
Incubation Time:

4 h
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.

Western Blot Analysis^[1]

Cell Line:

H358 nonsmall cell lung cancer cells
Concentration:

2 μM
Incubation Time:

2, 4, 6, 8 h
Result:

Induced substantial NSD2 degradation within 2 h, eliminating ~70% of protein.
Achieved maximal degradation by 4 h.

Western Blot Analysis^[1]

Cell Line:

PC3 prostate cancer cells
Concentration:

10 μM
Incubation Time:

4 h
Result:

Induced significant degradation of NSD2 at 10 μM.
No apparent degradation was observed with a comparator degrader at the same concentration.

Western Blot Analysis^[1]

Cell Line:

H358 nonsmall cell lung cancer cells
Concentration:

2 μM
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.

Western Blot Analysis^[1]

Cell Line:

H358 nonsmall cell lung cancer cells
Concentration:

2.5, 5 μM
Incubation Time:

4 h
Result:

Maintained comparable NSD2 degradation efficiency in both oxidase-free Opti-MEM and complete RPMI1640+10%FBS media.

Western Blot Analysis^[1]

Cell Line:

FBXO22 knockout 293T cells
Concentration:

2 μM
Incubation Time:

4 h
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.

Cell Migration Assay ^[1]

Cell Line:

PC3 prostate cancer cells
Concentration:

1, 5, 10 μM
Incubation Time:

24 h
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

CAS. Nr. 3108071-48-0
Molecular Weight 642.70
Formel C₃₈H₃₄N₄O₆
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Tang H, et al. Aryl Aldehyde-Anchored Small Molecules Recruit FBXO22 for Targeted Degradation of NSD2. Journal of medicinal chemistry. 2026 Jul 09;69(13):15317-15338. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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PROTAC NSD2 degrader-1

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PROTAC NSD2 degrader-1 Related Classifications

HY-184968 Related Classifications