AC-73

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AC-73 是 Cluster of Differentiation 147 (CD147) 的第一种特定的口服生物利用的抑制剂，可特异性破坏 CD147 的二聚化 (结合位点在 CD147 的 N 端 IgC2 域中包括 Glu64 和 Glu73)，从而抑制 CD147/ERK1/2/STAT3/MMP-2 途径，并抑制肝癌细胞的运动和侵袭。AC-73 还是一种抗增殖药，也是白血病细胞自噬的诱导剂。

AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells.

AC-73 (5-10 μM; 24 hours; SMMC-7721 and Huh-7 cells) treatment significantly decreases the migration ability of SMMC-7721 and Huh-7 cells in a dose-dependent manner and decreases the invasion of two HCC cells in a dose-dependent manner at 24 hours. AC-73 treatment reduces HCC metastases. There are no obvious effects on cell viability when two HCC cells are treated with AC-73 at a maximum concentration of 20 μM. The possible binding sites of AC-73 on CD147 included Glu64 and Glu73 in the N-terminal IgC2 domain, which two residues are located in the dimer interface of CD147. AC-73 (5-10 μM; 24 hours; SMMC-7721 cells) treatment could significantly inhibit both MMP-2 and MMP-9 mRNA expression at the concentration of 10 μM, especially MMP-2, but no obvious effect on MMP-1, MMP-3, MMP-7, MMP-11 nor MMP-13. AC-73 could dose dependently reduce the expression of MMP-2 mRNA level and secretion of the protein level using RT-qPCR analysis and gelatin zymography experiments.AC-73 (5-20 μM; 6 hours; SMMC-7721 cells) treatment dose-dependently suppresses the phosphorylation of ERK1/2 and STAT3.RT-PCR Cell Line:SMMC-7721 cells Concentration:5 μM or 10 μM Incubation Time:24 hours Result:Significantly inhibited both MMP-2 and MMP-9 mRNA expression at the concentration of 10 μM. Dose dependently reduced the expression of MMP-2 mRNA level and secretion of the protein level using RT-qPCR analysis and gelatin zymography experiments.Western Blot Analysis Cell Line:SMMC-7721 cells Concentration:5 μM, 10 μM or 20 μM Incubation Time:6 hours Result:The phosphorylation of ERK1/2 and STAT3 was dose-dependently suppressed.

AC-73 (25-50 mg/kg; for 4 weeks; Male BALB/c nu/nu mice) treatment significantly decreases the incidence of metastatic foci in nude mice. AC-73 inhibits the phosphorylation of ERK1/2 and STAT3 in a dose-dependent manner. MMP-2 is also reduced by AC-73. AC-73 could not inhibit tumor cell proliferation in vivo.Animal Model:Male BALB/c nu/nu mice (4-6 weeks) with SMMC-7721 cellsDosage:25 mg/kg, 50 mg/kg Administration: Injected; daily; for 3 weeks Result:Significantly decreased the incidence of metastatic foci in nude mice. Inhibited the phosphorylation of ERK1/2 and STAT3 in a dose-dependent manner. MMP-2 was also reduced.

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Autophagy

Autophagy

Autophagy

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775294-71-8

319.4

C21H21NO2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 250 mg/mL (782.72 mM )

OC(CNCc1ccc(cc1)-c1ccccc1)c1cccc(O)c1

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(-20℃)

With Ice Pack

≥ 2 years