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BRD4/NAMPT-IN-1

CAS No. :

MCE 國(guó)際站：BRD4/NAMPT-IN-1

產(chǎn)品活性：BRD4/NAMPT-IN-1 (Compound A2) 對(duì) NAMPT 和 BRD4 有較強(qiáng)的抑制作用 (IC₅₀=35 nM (NAMPT) 和 58 nM (BRD4))。BRD4/NAMPT-IN-1顯著抑制肝癌細(xì)胞的生長(zhǎng)和遷移，促進(jìn)細(xì)胞凋亡。BRD4/NAMPT-IN-1在 HCCLM3 異種移植小鼠模型中也表現(xiàn)出強(qiáng)大的抗癌作用，沒有明顯的毒性作用。

研究領(lǐng)域：Metabolic Enzyme/Protease  |  Epigenetics

作用靶點(diǎn)：NAMPT  |  Epigenetic Reader Domain

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.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.
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.
BRD4/NAMPT-IN-1 (1-10 μM; 72 h) dose-dependently reduces NAD ⁺ concentration in Hep3B cells and HCCLM3 cells.

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.

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