Bioactivity | Laccaic acid A is a orally active and DNA-competitive inhibitor of DNA methyltransferase 1 (Dnmt1) (Ki=310 nM; IC50=650 nM). Laccaic acid A has stronger Dnmt1 inhibitory effect than SG-1027 (HY-13962). Laccaic acid A combined with Phenethyl isothiocyanate has a strong synergistic effect on colorectal cancer[1][2]. |
Invitro | Laccaic acid A (200 μM) 与 0.5 μM Decitabine (HY-A0004) 协同改变 MCF-7 乳腺癌细胞中甲基化基因的表达[1]。Laccaic acid A (0.01-100 μM; 24 h, 48 h, and 72 h) 抑制人直肠癌细胞 HT29 的生长,处理 72 h 时,IC50 为 6.08 μM[2]。Laccaic acid A (6.08 μM) 诱导 HT29 细胞凋亡,并将细胞周期阻滞在亚 G1 期[2]。 |
In Vivo | Laccaic acid A (50 mg/kg,100 mg/kg,200 mg/kg; 口服; 每天 1 次,共 21 天) 对大鼠直肠癌模型具有改善效果[2]。 Animal Model: |
Name | Laccaic acid A |
CAS | 15979-35-8 |
Formula | C26H19NO12 |
Molar Mass | 537.43 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Fagan RL, et al. Laccaic acid A is a direct, DNA-competitive inhibitor of DNA methyltransferase 1. J Biol Chem. 2013 Aug 16;288(33):23858-67. [2]. Gupta R, et al. Potent antitumor activity of Laccaic acid and Phenethyl isothiocyanate combination in colorectal cancer via dual inhibition of DNA methyltransferase-1 and Histone deacetylase-1. Toxicol Appl Pharmacol. 2019 Aug 15;377:114631. |