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.
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- Fòrmula: C46H43N7O9
- Peso molecular:837.88
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Almacenamiento:
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
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Actividad biológica
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Chemical Information
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
eRF3a/GSPT1 18 nM (DC50) |
NSD2 >10 μM (DC50) |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| VCaP | IC50 |
0.13 μM
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Inhibition of VCaP cell viability incubated 7 days by CellTiter-Glo assay.
Inhibition of VCaP cell viability incubated 7 days by CellTiter-Glo assay.
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42911699 |
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VCaP and MM.1S cells
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Concentration:2 μM; 0.001, 0.01, 0.1, 1, 10 μM (VCaP); 0.008, 0.04, 0.2, 1, 5 μM (MM.1S)
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Incubation Time:24 h
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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.
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Cell Line:VCaP cells
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Concentration:2 μM
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Incubation Time:24 h
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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.
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Cell Line:VCaP cells
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Concentration:Two-fold serial dilution, highest 30 μM
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Incubation Time:7 days
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Result:Inhibited VCaP cell viability with IC50 = 0.13 μM.
Chemical Information
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Peso molecular 837.88
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Fòrmula C46H43N7O9
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
424-GD Related Classifications
HY-190751 Related Classifications
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