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Cat. No.: HY-190750

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424-ND

424-ND is a selective NSD2 PROTAC degrader (DC₅₀ 1 µM). 424-ND binds to CRBN and induces ubiquitination and proteasomal degradation of NSD2. 424-ND inhibits Androgen receptor signaling. 424-ND can be used for research on prostate cancer and multiple myeloma.
(Pink: NSD2 Target protein ligand; Blue: Cereblon ligand (HY-W087383); Black: linker).

For research use only. We do not sell to patients.

CAS No.: 3070841-14-1
Formula: C₄₅H₄₀FN₇O₉
Molecular Weight:841.84

Storage:

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

Data Sheet (277 KB)

424-ND Chemical Structure

CAS No.: 3070841-14-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

424-ND is a selective NSD2 PROTAC degrader (DC₅₀ 1 µM). 424-ND binds to CRBN and induces ubiquitination and proteasomal degradation of NSD2. 424-ND inhibits Androgen receptor signaling. 424-ND can be used for research on prostate cancer and multiple myeloma^[1]. (Pink: NSD2 Target protein ligand; Blue: Cereblon ligand (HY-W087383); Black: linker).

IC₅₀ & Target

^[1]

NSD2

1 μM (DC₅₀)

eRF3a/GSPT1

>10 μM (DC₅₀)

Cereblon

All PROTACs Isoforms :

All Histone Methyltransferase Isoforms :

All Eukaryotic Release Factor (eRF) Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
VCaP	IC50	30 μM	Cell viability against human VCaP cells assessed by CellTiter-Glo after 7 days of incubation with two-fold serial dilutions, with IC50 greater than 30 μM. Cell viability against human VCaP cells assessed by CellTiter-Glo after 7 days of incubation with two-fold serial dilutions, with IC50 greater than 30 μM.	42911699

In Vitro

Anti-cancerProtein/Amino Acid MetabolismOthers

Anti-cancer

Protein/Amino Acid Metabolism

424-ND (0.001-10 µM VCaP; 0.008-5 µM MM.1S; 24 h) selectively degrades NSD2 without affecting GSPT1 in VCaP and MM.1S cells, achieving 97% NSD2 degradation and 0% GSPT1 degradation at 2 µM in VCaP cells^[1].

Protein/Amino Acid Metabolism

424-ND exhibits selective degradation potency against NSD2 (DC₅₀ 1 µM), superior to its degradation potency against GSPT1 (DC₅₀ > 10 µM)^[1].
424-ND (2 µM; 6-8 h) selectively reduces NSD2 protein in VCaP cells via TMT proteomics without causing widespread off-target degradation^[1].
424-ND (2 µM; 14 days) maintains NSD2 degradation in VCaP cells under prolonged exposure and inhibits AR downstream gene expression^[1].

Others

424-ND binds CRBN with nanomolar affinity and exhibits positive ternary cooperativity with NSD2 (α = 2.00), whereas it shows no positive ternary cooperativity with GSPT1 (α < 1)^[1].
424-ND (maximum concentration 30 µM; 7 days) shows a weak effect on VCaP cell viability (IC₅₀ > 30 µM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

VCaP and MM.1S cells
Concentration:

0.001, 0.01, 0.1, 1, 10 µM (VCaP); 0.008, 0.04, 0.2, 1, 5 µM (MM.1S); 2 µM (VCaP table)
Incubation Time:

24 h
Result:

In VCaP and MM.1S, NSD2-L and NSD2-S decreased dose-dependently, whereas GSPT1 remained unchanged.
At 2 µM for 24 h in VCaP, 97% NSD2 degradation and 0% GSPT1 degradation were observed.

Cell Viability Assay^[1]

Cell Line:

VCaP cells
Concentration:

Two-fold serial dilution; highest concentration 30 µM
Incubation Time:

7 days
Result:

IC₅₀ was > 30 µM in VCaP cells.

Western Blot Analysis^[1]

Cell Line:

VCaP cells
Concentration:

2 µM
Incubation Time:

14 days
Result:

NSD2 protein levels remained markedly decreased, GSPT1 remained unchanged, and FKBP5 and KLK3 expression was substantially decreased.

Related Protocols :

Research Protocol for Endocrine Diseases

Chemical Information

CAS No. 3070841-14-1
Molecular Weight 841.84
Formula C₄₅H₄₀FN₇O₉
SMILES

O=C1C(CCC(N1)=O)N2C(C3=C(C=C(F)C(N(CC4)CCC4NC(C(C=C5)=CC=C5NC(C6=CC=C(CN(C(C(C=C7OC8)=CC=C7NC8=O)=O)C9CC9)C=C6)=O)=O)=C3)C2=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Shen W, et al. Single-Atom Modification Enables Reversal of Degradation Selectivity between NSD2 and GSPT1. Journal of medicinal chemistry. 2026 Oct 22;69(20):24137-24149. [Content Brief]

Calculators

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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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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424-ND

All PROTACs Isoforms

All Histone Methyltransferase Isoforms

All Eukaryotic Release Factor (eRF) Isoforms