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.

For research use only. We do not sell to patients.

BRD4/NAMPT-IN-1 Chemical Structure

BRD4/NAMPT-IN-1 Chemical Structure

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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
Unlabeled Cas

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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BRD4/NAMPT-IN-1 Related Classifications

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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-1NAMPTEpigenetic 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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