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Cat. No.: HY-190751

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424-GD

424-GD is a selective GSPT1 PROTAC degrader (DC₅₀ = 18 nM). 424-GD recruits CRBN and induces GSPT1 ubiquitination and degradation. 424-GD induces the integrated stress response. 424-GD can be used for research on prostate cancer and multiple myeloma.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Formule: C₄₆H₄₃N₇O₉
Masse moléculaire:837.88

Stockage:

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

424-GD Chemical Structure

Stock

Quantité

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

eRF3a/GSPT1

18 nM (DC₅₀)

NSD2

>10 μM (DC₅₀)

Cereblon

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Cellular Effect

Cell Line	Type	Value	Description	References
VCaP	IC50	0.13 μM	Inhibition of VCaP cell viability incubated 7 days by CellTiter-Glo assay. Inhibition of VCaP cell viability incubated 7 days by CellTiter-Glo assay.	42911699

In Vitro

Anti-cancerProtein/Amino Acid MetabolismOthers

Anti-cancer

424-GD (up to 30 μM; 7 days) potently inhibits VCaP cell viability with an IC₅₀ of 0.13 μM^[1].

Anti-cancer

Protein/Amino Acid Metabolism

424-GD (2 μM; 24 h) is a selective GSPT1 degrader in VCaP and MM.1S cells, producing 99% GSPT1 degradation at 2 μM in VCaP cells, whereas NSD2 degradation is 43%^[1].
424-GD (2 μM; 24 h)-induced GSPT1 degradation in VCaP cells requires CRBN engagement and proteasome activity, but does not require NSD2 binding^[1].
424-GD (2 μM; 24 h) induces GSPT1 degradation and upregulates integrated stress response markers ATF4 and ATF3 in VCaP cells^[1].

Others

424-GD (30-3000 nM) binds to CRBN with a binary K_D of 0.16 μM and exhibits positive cooperativity with GSPT1 (α = 1.23), whereas its CRBN binding is attenuated in the presence of NSD2 (K_D = 0.56 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:

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

24 h
Result:

In VCaP cells at 2 μM for 24 h, NSD2 degradation was 43% and GSPT1 degradation was 99%.
In VCaP and MM.1S dose-response immunoblots, GSPT1 degradation was concentration-dependent with significantly lower potency toward NSD2.

Western Blot Analysis^[1]

Cell Line:

VCaP cells
Concentration:

2 μM
Incubation Time:

24 h
Result:

GSPT1 was degraded.
GSPT1 degradation was markedly attenuated by blockade of CRBN engagement or proteasome activity and was unaffected by blockade of NSD2 binding.\nDegraded GSPT1 and markedly increased ATF4 and ATF3 levels.

Cell Viability Assay^[1]

Cell Line:

VCaP cells
Concentration:

Two-fold serial dilution, highest 30 μM
Incubation Time:

7 days
Result:

Inhibited VCaP cell viability with IC₅₀ = 0.13 μM.

Chemical Information

Masse moléculaire 837.88
Formule C₄₆H₄₃N₇O₉
SMILES

O=C1C(CCC(N1)=O)N2C(C3=C(C=CC(N4CCC[C@H](CC4)NC(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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Keywords

MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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424-GD

Voir tous les produits spécifiques à Isoform PROTACs

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