BRD4/NAMPT-IN-1
Based on 1 Customer Validation
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 3049218-28-9
- Formula: C30H30ClN7O2S
- Molecular Weight:588.12
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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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Epigenetics Compound Library
HY-L005
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HY-L012
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HY-L024
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HY-L025
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HY-L036
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HY-L039
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HY-L079
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HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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BRD4(BD1BD2) 58 nM (IC50) |
BRD4 (BD1) 12 nM (IC50) |
BRD4 (BD2) 41 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCCLM3 | IC50 |
5.44 μM
Compound: A2
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Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs by MTT assay
Antiproliferative activity against human HCCLM3 cells incubated for 120 hrs by MTT assay
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[PMID: 38691889] |
| Hep 3B2 | IC50 |
2.37 μM
Compound: A2
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Antiproliferative activity against human Hep3B cells incubated for 120 hrs by MTT assay
Antiproliferative activity against human Hep3B cells incubated for 120 hrs by MTT assay
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[PMID: 38691889] |
| Huh-7 | IC50 |
6.49 μM
Compound: A2
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Antiproliferative activity against human Huh-7 cells incubated for 120 hrs by MTT assay
Antiproliferative activity against human Huh-7 cells incubated for 120 hrs by MTT assay
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[PMID: 38691889] |
| LX-2 | IC50 |
9.51 μM
Compound: A2
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Antiproliferative activity against human LX2 cells incubated for 120 hrs by MTT assay
Antiproliferative activity against human LX2 cells incubated for 120 hrs by MTT assay
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[PMID: 38691889] |
BRD4/NAMPT-IN-1 exhibits IC50 values of 12 nM for BRD4(BD1) and 41 nM for BRD4(BD2) against other members of the BET family[1].
BRD4/NAMPT-IN-1 inhibits the proliferation of cancer cells with IC50 of 2.37 μM (Hep3B), 6.49 μM (Huh7), 5.44 μM (HCCLM3) and 9.51 μM (LX-2), respectively[1].
BRD4/NAMPT-IN-1 (1-10 μM; 72 h) on Hep3B cells shows that: 1: it can inhibit the expression of oncogenes up-regulated by BRD4, and at the same time reduces the levels of NAPRT and NAMPT. 2: It significantly increases cell arrest at G0/G1 phase. 3: It dose-dependently induces apoptosis. 4: It dose-dependently inhibits the migratory ability of the cells[1].
BRD4/NAMPT-IN-1 (1-10 μM; 72 h) dose-dependently reduces NAD + concentration in Hep3B cells and HCCLM3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hep3B cells
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Concentration:1; 5; 10 μM
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Incubation Time:72 h
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Result:The apoptosis rate induced was significantly higher than that of the control FK866 (HY-50876) and JQ1 (HY-13030) at the same dose.
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Cell Line:Hep3B cells
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Concentration:1; 5; 10 μM
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Incubation Time:72 h
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Result:Significantly increased the accumulation of Hep3B cells at the G0/G1 stage over the commonly used hepatocellular carcinoma therapeutic agents FK866 (HY-50876) and JQ1 (HY-13030).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCCLM3 xenograft nude mice [1]
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Dosage:40 mg/kg/day and 80 mg/kg/day
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Administration:i.p.; 27day
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Result:Inhibited the growth of HCCLM3 tumors significantly in both groups at two different doses, with significant decreases in tumor volume and weight.
In the 40 mg/kg dose group, the tumor growth inhibition rate reached 37.20%, and in the 80 mg/kg dose group, the tumor growth inhibition rate reached 58.17%.
Showed no significant weight loss or other significant toxic side effects.
Chemical Information
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CAS No. 3049218-28-9
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Appearance Solid
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Molecular Weight 588.12
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Formula C30H30ClN7O2S
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Color White to off-white
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SMILES
ClC(C=C1)=CC=C1C2=N[C@@H](CC(NCCCNC(/C=C/C3=CN=CC=C3)=O)=O)C4=NN=C(C)N4C5=C2C(C)=C(C)S5
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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
DMSO : 100 mg/mL (170.03 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)
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 (4.25 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 (4.25 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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 1.7003 mL | 8.5017 mL | 17.0033 mL | 42.5083 mL |
| 5 mM | 0.3401 mL | 1.7003 mL | 3.4007 mL | 8.5017 mL | |
| 10 mM | 0.1700 mL | 0.8502 mL | 1.7003 mL | 4.2508 mL | |
| 15 mM | 0.1134 mL | 0.5668 mL | 1.1336 mL | 2.8339 mL | |
| 20 mM | 0.0850 mL | 0.4251 mL | 0.8502 mL | 2.1254 mL | |
| 25 mM | 0.0680 mL | 0.3401 mL | 0.6801 mL | 1.7003 mL | |
| 30 mM | 0.0567 mL | 0.2834 mL | 0.5668 mL | 1.4169 mL | |
| 40 mM | 0.0425 mL | 0.2125 mL | 0.4251 mL | 1.0627 mL | |
| 50 mM | 0.0340 mL | 0.1700 mL | 0.3401 mL | 0.8502 mL | |
| 60 mM | 0.0283 mL | 0.1417 mL | 0.2834 mL | 0.7085 mL | |
| 80 mM | 0.0213 mL | 0.1063 mL | 0.2125 mL | 0.5314 mL | |
| 100 mM | 0.0170 mL | 0.0850 mL | 0.1700 mL | 0.4251 mL |
BRD4/NAMPT-IN-1 Related Classifications
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