PROTAC NAMPT Degrader-32
PROTAC NAMPT Degrader-32 is a PROTAC degrader targeting NAMPT with an IC50 of 2.14 nM. PROTAC NAMPT Degrader-32 induces proteasome-dependent degradation of NAMPT and induces apoptosis in ovarian cancer cells (apoptosis). PROTAC NAMPT Degrader-32 can be used in research related to ovarian cancer.
(Pink: NAMPT ligand (HY-50876); Blue: VHL ligand (HY-112078); Black: linker (HY-W018678)).
For research use only. We do not sell to patients.
- Formula: C56H74N8O7S
- Molecular Weight:1003.30
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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
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- References
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
30.6 nM
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Antiproliferative activity against human A2780 ovarian cancer cells assessed as inhibition of cell proliferation.
Antiproliferative activity against human A2780 ovarian cancer cells assessed as inhibition of cell proliferation.
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37369332 |
| HUVEC | IC50 |
0.30 μM
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Antiproliferative activity against human umbilical vein endothelial cells (HUVEC) assessed as inhibition of cell proliferation.
Antiproliferative activity against human umbilical vein endothelial cells (HUVEC) assessed as inhibition of cell proliferation.
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37369332 |
In Vitro
PROTAC NAMPT Degrader-32 (compound C5) potently inhibits recombinant NAMPT enzyme activity with an IC50 of 2.14 nM[1].
PROTAC NAMPT Degrader-32 (250-500 nM; 24 h) effectively degrades NAMPT in A2780 cells with a DC50 of 31.7 nM[1].
PROTAC NAMPT Degrader-32 (200 nM; 1-24 h) induces time-dependent NAMPT degradation in A2780 cells[1].
PROTAC NAMPT Degrader-32 (200 nM)-induced NAMPT degradation in A2780 cells is proteasome-dependent[1].
PROTAC NAMPT Degrader-32-induced NAMPT degradation in A2780 cells is VHL-dependent[1].
PROTAC NAMPT Degrader-32 inhibits A2780 cell proliferation with an IC50 of 30.6 nM and exhibits reduced cytotoxicity against HUVEC cells with an IC50 of 0.30 μM[1].
PROTAC NAMPT Degrader-32 (1.6-1000 nM; 48 h) induces apoptosis in A2780 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780
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Concentration:250 or 500 nM
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Incubation Time:24 h
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Result:Induced significant NAMPT degradation at both 500 nM and 250 nM.
Exhibited the most potent degradation activity with a DC50 value of 31.7 nM.
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Cell Line:A2780
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Concentration:200 nM
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Incubation Time:1, 2, 4, 6, 12, 18 and 24 h
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Result:Degraded NAMPT in a time-dependent manner.
Achieved approximately 78% degradation of NAMPT after 24 h.
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Cell Line:A2780
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Concentration:1.6, 40 and 1000 nM
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Incubation Time:48 h
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Result:Concentration-dependently induced apoptosis.
Increased apoptotic rates from 10.15% to 20.81% over the concentration range of 1.6 nM to 1 μM.
Chemical Information
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Molecular Weight 1003.30
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Formula C56H74N8O7S
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SMILES
O=C([C@@H](NC(CCCCCCCNC(C1=CC=C(C(N2CCC(CC2)CCCCNC(/C=C/C3=CC=CN=C3)=O)=O)C=C1)=O)=O)C(C)(C)C)N4C[C@@H](C[C@H]4C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)O
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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-32 Related Classifications
HY-155506 Related Classifications
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