PROTAC NAMPT Degrader-30
Based on 1 Customer Validation
PROTAC NAMPT Degrader-30 is a PROTAC degrader targeting nicotinamide phosphoribosyltransferase (NAMPT), with a DC50 of 8.4 nM in A2780 cells. PROTAC NAMPT Degrader-30 binds to the VHL E3 ligase and forms a ternary complex with NAMPT, which induces ubiquitination and subsequent proteasomal degradation of NAMPT, thereby inhibiting the enzymatic activity of NAMPT. PROTAC NAMPT Degrader-30 reduces intracellular NAD+ levels and suppresses tumor cell proliferation. PROTAC NAMPT Degrader-30 exhibits a fluorescence turn-on response to the NAMPT protein, enabling real-time visualization of the NAMPT degradation process in living cells. PROTAC NAMPT Degrader-30 is applicable for research on ovarian cancer.
(Pink: NAMPT ligand (HY-187006); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.41%
- CAS No.: 3035008-40-0
- Formula: C59H73N9O7S
- Molecular Weight:1052.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Nampt 8.4 nM (DC50) |
Nampt 41.9 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
12.1 nM
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Antiproliferative activity against human ovarian cancer A2780 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human ovarian cancer A2780 cells assessed by CCK-8 assay after 72 h incubation.
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36442664 |
In Vitro
PROTAC NAMPT Degrader-30 potently inhibits purified NAMPT enzyme with an IC50 of 41.9 nM[1].
PROTAC NAMPT Degrader-30 (50-1000 nM) is an environmentally sensitive fluorescent molecule with turn-on fluorescence response to NAMPT protein[1].
PROTAC NAMPT Degrader-30 (10 μM; 2 h) directly binds to both NAMPT and VHL in intact A2780 cells, confirming ternary complex formation[1].
PROTAC NAMPT Degrader-30 (Compound B4) (1-500 nM; 24 h) potently degrades endogenous NAMPT in A2780 cells in a dose-dependent manner with a DC50 of 8.4 nM[1].
PROTAC NAMPT Degrader-30 exhibits potent antiproliferative activity against A2780 ovarian cancer cells with an IC50 of 12.1 nM[1].
PROTAC NAMPT Degrader-30 (30 nM; 1-24 h) degrades NAMPT in A2780 cells in a time-dependent manner across 24 h of treatment[1].
PROTAC NAMPT Degrader-30 (4.1-1000 nM; 24 h) potently reduces intracellular NAD+ production in A2780 cells at sub-10 nM concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human ovarian cancer A2780 cells
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Concentration:1-500 nM
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Incubation Time:24 h
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Result:Degrades NAMPT in A2780 cells in a dose-dependent manner within the 1-30 nM concentration range, achieving a half-maximal NAMPT degradation (DC50) value of 8.4 nM.
Shows decreased NAMPT degradation efficacy at concentrations higher than 50 nM, and full loss of degradation ability at concentrations greater than 5 μM, corresponding to the hook effect.
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Cell Line:Human ovarian cancer A2780 cells
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Concentration:30 nM
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Incubation Time:1 h; 2 h; 4 h; 8 h; 24 h
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Result:Initiates NAMPT degradation as early as 1 h after incubation, and NAMPT protein levels continue to decrease progressively over the full 24 h incubation period in a strictly time-dependent manner.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-∞ | MRT0-t |
|---|---|---|---|---|---|---|---|
| Rat[1] | 30 mg/kg | i.p. | 9.89 h | 4 h | 175.47 ng/mL | 1111.92 ng·h/mL | 12.67 h |
In Vivo
PROTAC NAMPT Degrader-30 (30 mg/kg; i.p.; single dose) provides sustained plasma exposure above the NAMPT degradation threshold with a 9.89 h T1/2 in Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude female mice, 4-5 weeks of age, weighing 14-18 g[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; once daily; 14 consecutive days
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Result:Achieved 53% tumor growth inhibition at 10 mg/kg.
Achieved 73% tumor growth inhibition at 30 mg/kg.
Reduced intratumoral NAMPT protein levels significantly at 30 mg/kg.
Verified pronounced NAMPT degradation at 30 mg/kg.
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Animal Model:Sprague-Dawley male rats, 6-8 weeks old, body weight 180-220 g[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose
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Result:Reached a plasma half-life of 9.89 h.
Reached a peak plasma concentration Cmax of 175 ng/mL (166 nM) that exceeds the cellular DC50 value.
Chemical Information
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CAS No. 3035008-40-0
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Appearance Solid
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Molecular Weight 1052.33
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Formula C59H73N9O7S
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Color Light yellow to yellow
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SMILES
O=C(C(C1=CC=C(C=C1)C(NCC2=CN=CC=C2)=O)=NC3=C4C=C(C=C3)NC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)N4CCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (95.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9503 mL | 4.7514 mL | 9.5027 mL | 23.7568 mL |
| 5 mM | 0.1901 mL | 0.9503 mL | 1.9005 mL | 4.7514 mL | |
| 10 mM | 0.0950 mL | 0.4751 mL | 0.9503 mL | 2.3757 mL | |
| 15 mM | 0.0634 mL | 0.3168 mL | 0.6335 mL | 1.5838 mL | |
| 20 mM | 0.0475 mL | 0.2376 mL | 0.4751 mL | 1.1878 mL | |
| 25 mM | 0.0380 mL | 0.1901 mL | 0.3801 mL | 0.9503 mL | |
| 30 mM | 0.0317 mL | 0.1584 mL | 0.3168 mL | 0.7919 mL | |
| 40 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5939 mL | |
| 50 mM | 0.0190 mL | 0.0950 mL | 0.1901 mL | 0.4751 mL | |
| 60 mM | 0.0158 mL | 0.0792 mL | 0.1584 mL | 0.3959 mL | |
| 80 mM | 0.0119 mL | 0.0594 mL | 0.1188 mL | 0.2970 mL |
PROTAC NAMPT Degrader-30 Related Classifications
HY-152154 Related Classifications
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