PROTAC NAMPT Degrader-28
PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research.
(Pink: NAMPT ligand (HY-181881); Blue: VHL ligand (HY-112078); Black: linker (HY-W018678)).
For research use only. We do not sell to patients.
- Formula: C58H73N9O6S
- Molecular Weight:1024.32
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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
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Biological Activity
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VHL |
PROTAC NAMPT Degrader-28 (Compound U42) (5 nM-4 μM; 1 h) inhibits the catalytic activity of recombinant mouse NAMPT, with an IC50 of 417.5 nM[1].
PROTAC NAMPT Degrader-28 (10 nM-1 μM; 72 h) potently reduces the viability of MCF7 and 4T1cl5 breast cancer cells, with IC50 values of 110 nM and 157 nM, respectively[1].
PROTAC NAMPT Degrader-28 (300 nM; 24 h, 48 h) significantly reduces intracellular NAD+ levels in MCF7 and 4T1cl5 breast cancer cells after 24 h and 48 h of treatment[1].
PROTAC NAMPT Degrader-28 (1-3 μM; 8 days) inhibits mammosphere formation in 3D breast cancer cell cultures, induces NAMPT degradation, and reduces extracellular NAMPT levels after 8 days of treatment[1].
PROTAC NAMPT Degrader-28 (10 μM; 5 h) stabilizes NAMPT and VHL proteins against thermal denaturation in MCF7 and 4T1cl5 breast cancer cells, confirming the formation of a ternary complex among PROTAC NAMPT Degrader-28, NAMPT, and VHL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 human breast cancer cells, 4T1cl5 murine triple-negative breast cancer cells
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Concentration:0.03, 0.1, 0.3, 0.6 and 1 μM; 300 nM (with bortezomib pre-treatment for 30 min; with inhibitor 7 or VHL-Ac pre-treatment for 1 h)
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Incubation Time:18 h
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Result:Induced NAMPT degradation in a dose-dependent manner, with DC50 values of 45 nM in MCF7 cells and 55 nM in 4T1cl5 cells.
Blocked NAMPT degradation when co-treated with bortezomib.
Abolished NAMPT degradation when pre-treated with inhibitor 7 or VHL-Ac in both cell lines.
Did not affect NAPRT protein levels in either cell line.
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Cell Line:MCF7 human breast cancer cells, 4T1cl5 murine triple-negative breast cancer cells
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Concentration:10 nM, 30, 100, 300, 600 and 1 μM
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Incubation Time:72 h
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Result:Reduced cell viability with IC50 values of 110 nM in MCF7 cells and 157 nM in 4T1cl5 cells.
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Cell Line:MCF7 human breast cancer cells, 4T1cl5 murine triple-negative breast cancer cells
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Concentration:0.1. 0.3, 1 and 3 μM
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Incubation Time:18 h (complete medium) followed by 18 h (serum-free medium)
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Result:Induced dose-dependent degradation of eNAMPT in both cell lines, with significant reductions observed at 0.1, 0.3, and 1 μM.
Chemical Information
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Molecular Weight 1024.32
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Formula C58H73N9O6S
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SMILES
O=C(NCCCCCCCN1N=NC(C2=CC=CN=C2)=C1)C3=CC=CC=C3C4=CC(OCCCCCCCC(N[C@H](C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C=C6)C7=C(N=CS7)C)C)=O)=O)C(C)(C)C)=O)=CC=C4
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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 NAMPT Degrader-28 Related Classifications
HY-181880 Related Classifications
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