2. Metabolic Enzyme/Protease Epigenetics
  3. NAMPT Epigenetic Reader Domain
  4. BRD4/NAMPT-IN-1

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.

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BRD4/NAMPT-IN-1 Chemical Structure

BRD4/NAMPT-IN-1 Chemical Structure

CAS No. : 3049218-28-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 323 In-stock
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10 mg USD 400 In-stock
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Based on 1 publication(s) in Google Scholar

BRD4/NAMPT-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

BRD4(BD1BD2)

58 nM (IC50)

BRD4 (BD1)

12 nM (IC50)

BRD4 (BD2)

41 nM (IC50)

In Vitro

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.

BRD4/NAMPT-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Hep3B cells
Concentration: 1; 5; 10 μM
Incubation Time: 72 h
Result: The apoptosis rate induced was significantly higher than that of the control FK866 (HY-50876) and JQ1 (HY-13030) at the same dose.

Cell Cycle Analysis[1]

Cell Line: Hep3B cells
Concentration: 1; 5; 10 μM
Incubation Time: 72 h
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).
In Vivo

BRD4/NAMPT-IN-1 (i.p.; 40 mg/kg/day and 80 mg/kg/day; 27 days) exhibits dose-dependent tumor suppression in HCCLM3 xenograft nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HCCLM3 xenograft nude mice [1]
Dosage: 40 mg/kg/day and 80 mg/kg/day
Administration: i.p.; 27day
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.
Molecular Weight

588.12

Formula

C30H30ClN7O2S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
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 (170.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7003 mL 8.5017 mL 17.0033 mL
5 mM 0.3401 mL 1.7003 mL 3.4007 mL
View the 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.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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BRD4/NAMPT-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD4/NAMPT-IN-13049218-28-9NAMPTEpigenetic Reader DomainNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorDual InhibitorCell Cycle ArrestApoptosisAnti-migratory EffectTumor Growth InhibitionNAD+ Metabolism Inhibition,HCCLM3Inhibitorinhibitorinhibit

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