LYP-8
Based on 1 Customer Validation
LYP-8 is an intracellular nicotinamide phosphoribosyltransferase (iNAMPT) inhibitor with an IC50 of 0.76 μM, a reducing agent, and a tumor growth inhibitor. LYP-8 recruits VHL E3 ligase to induce iNAMPT polyubiquitination and proteasome-dependent degradation, and inhibits iNAMPT enzymatic activity. LYP-8 reduces eNAMPT levels by degrading iNAMPT to decrease eNAMPT secretion. LYP-8 reduces intracellular NAD+ levels in cancer cells and proinflammatory cytokine levels (IL-6, TNF-α) in tumor tissue and serum. LYP-8 can be used for the research of colon cancer.
(Pink: NAMPT ligand (HY-50876); Blue: VHL ligand (HY-112078); Black: linker (HY-128801)).
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- Pureté: 99.89%
- CAS No.: 2484876-99-3
- Formule: C56H74N8O10S
- Masse moléculaire:1051.30
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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iNAMPT 0.76 μM (IC50) |
LYP-8 (0.5-5 μM; 24 h) potently degrades iNAMPT in human ovarian cancer cell line SKOV-3, with degradation rates reaching 97% and 96% at concentrations of 0.5 μM and 5 μM respectively after 24 h of treatment[1].
LYP-8 (0.01-5 μM; 24 h) induces dose-dependent degradation of iNAMPT in SKOV-3, MKN-45 and CT-26 cells, with DC50 values of 26 nM, 6.8 nM and 520 nM respectively after 24 h of treatment[1].
LYP-8 (50 nM-5 μM; 2-24 h) induces time-dependent degradation of iNAMPT in SKOV-3, MKN-45 and CT-26 cells. Downregulation of iNAMPT expression is detectable as early as 2 h in SKOV-3 cells, and iNAMPT is almost completely depleted after 24 h[1].
LYP-8 (50-100 nM; 24 h) induces iNAMPT degradation in SKOV-3 and MKN-45 cells via a mechanism that depends on binding to VHL and NAMPT and is mediated by the proteasome pathway[1].
LYP-8 (60 min) potently inhibits NAMPT enzymatic activity in cell-free biochemical assays, with an IC50 value of 0.76 μM[1].
Treatment with LYP-8 (0.1-5 μM; 24 h) induces dose-dependent degradation of intracellular iNAMPT and secreted eNAMPT in mouse colorectal cancer CT-26 cells and human ovarian cancer SKOV-3 cells[1].
LYP-8 exhibits cytotoxicity against murine colorectal cancer CT-26 cells (IC50 = 25.8 μM) and human ovarian cancer SKOV-3 cells (IC50 = 1.02 μM) following 72 h of treatment[1].
LYP-8 (100 nM; 24 h) significantly reduces intracellular NAD+ levels in SKOV-3 human ovarian cancer cells in a dose-dependent manner, with a treatment duration of 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | AUC0-24 | T1/2 | Vz/F |
|---|---|---|---|---|---|---|---|
| Rat[1] | 14 mg/kg | i.p. | 1 h | 147.3 ng/mL | 919 ng·h/mL | 22 h | 483422 mL/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6 weeks old, subcutaneously injected with 2×105 CT-26 murine colorectal cancer cells)[1]
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Dosage:20 mg/kg
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Administration:i.p.; once a day; 30 days
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Result:Achieved a tumor growth inhibition (TGI) value of 46%.
Degraded iNAMPT in tumor tissue.
Reduced serum levels of proinflammatory cytokines IL-6 and TNF-α.
Did not induce substantial body weight loss.
Resulted in a significant decrease in spleen size and spleen index compared to FK866.
Showed no abnormal histological appearance of liver tissue via H&E staining, indicating no liver toxicity at the tested dose.
Chemical Information
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CAS No. 2484876-99-3
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Appearance Solid
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Masse moléculaire 1051.30
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Formule C56H74N8O10S
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Color White to off-white
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C4=CC=C(C=C4)C(N5CCC(CC5)CCCCNC(/C=C/C6=CN=CC=C6)=O)=O)=O)=O)=O)O)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (95.12 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 0.9512 mL | 4.7560 mL | 9.5120 mL | 23.7801 mL |
| 5 mM | 0.1902 mL | 0.9512 mL | 1.9024 mL | 4.7560 mL | |
| 10 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3780 mL | |
| 15 mM | 0.0634 mL | 0.3171 mL | 0.6341 mL | 1.5853 mL | |
| 20 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1890 mL | |
| 25 mM | 0.0380 mL | 0.1902 mL | 0.3805 mL | 0.9512 mL | |
| 30 mM | 0.0317 mL | 0.1585 mL | 0.3171 mL | 0.7927 mL | |
| 40 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5945 mL | |
| 50 mM | 0.0190 mL | 0.0951 mL | 0.1902 mL | 0.4756 mL | |
| 60 mM | 0.0159 mL | 0.0793 mL | 0.1585 mL | 0.3963 mL | |
| 80 mM | 0.0119 mL | 0.0595 mL | 0.1189 mL | 0.2973 mL |
LYP-8 Related Classifications
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