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1A-116

CAS No. : 1430208-73-3

MCE 国际站：1A-116

产品活性：1A-116 是一种对 W56 残基具有特异性的 Rac1 抑制剂，能有效防止 EGF 诱导的 Rac1 激活，并阻断 Rac1-P-Rex1 的相互作用。1A-116 能以昼夜节律依赖的方式诱导细胞凋亡并抑制细胞的增殖、迁移和周期进展。1A-116 在体内也具有较高的抗癌细胞转移活性。

研究领域：GPCR/G Protein  |  Apoptosis

作用靶点：Ras  |  Apoptosis

In Vitro: 1A-116 (48 h) inhibits F3II and MDA-MB-231 cells proliferation in a concentration-dependent manner with IC₅₀s of 4 μM and 21 μM, respectively.
?1A-116 (1, 10 μM; 12 h) dramatically impaires Rac1 activation, and reduces Rac1-GTP intracellular levels in a concentration-dependent manner in F3II cells.
?1A-116 (50, 100 μM; 12 h) blocks Rac1-P-Rex1 interaction.
?1A-116 (20 μM; 5 h intervals over 25 h) inhibits LN229 cells proliferation in a circadian manner.
?1A-116 (10 μM; 16 h) significantly reduces cell migration at 10 HPS which exhibits temporal dependence. (HPS: After the serum shock, the elapsed time (in hours) is recorded as the hours post-synchronization (HPS)).
?1A-116 (20, 50 μM; 6 h) induces cells apoptosis and in a circadian-dependent manner.
?1A-116 (100 nM) decreases the thickness of the epidermal layers of Vav2 and Rac1-mediated hyperplasia, but not the PAK1-mediated one, which exhibits the activity of inhibiting Rac1 at the GEF-Rac1 level.

In Vivo: 1A-116 (3 mg/kg; i.v.; once a day for 21 days) demonstrates a high antimetastatic activity with about 60% formation reduction of total metastatic lung colonies in vivo and shows no apparent toxicity.
?1A-116 (20 mg/kg; i.p.; once a day, 73 days for ZT12, 68 days for ZT3) increases survival time when treated at ZT12 compare to ZT3 in tumor-bearing mice. (ZT: Zeitgeber time 12 (ZT12) defined as the time of lights off (local time 7 p.m.) and ZT0 defined as lights on (local time 7 a.m.)).
?1A-116 shows good oral availability.

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