SIRT6 activator 12q is a selective SIRT6 activator (IC₅₀ = 0.58μM). SIRT6 activator 12q exhibits an IC₅₀ of 171.20μM against SIRT1, while its IC₅₀ values for SIRT2, SIRT3, and SIRT5 are all greater than 200μM. SIRT6 activator 12q demonstrates significant anticancer activity and can be used in cancer-related research[1-2].
In vitro, SIRT6 activator 12q (2.5–10μM) was used to treat human pancreatic ductal adenocarcinoma (PDAC) cell lines, including PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1, for 24–72 hours. SIRT6 activator 12q significantly inhibited cell proliferation and migration in a concentration‑dependent manner. SIRT6 activator 12q induced G2‑phase cell cycle arrest and apoptosis, reduced the acetylation levels of histone H3K9, H3K18, and H3K56, and downregulated the expression of Lin28b and IGF2BP3[1].
In vivo, SIRT6 activator 12q (10mg/kg/day) was administered orally to nude mice bearing PANC‑1 xenograft tumors for 28 days. SIRT6 activator 12q significantly suppressed tumor growth, induced tumor cell apoptosis, and decreased the expression of Lin28b in tumor tissues[1].
SIRT6 activator 12q是一种SIRT6选择性激活剂（IC50=0.58μM）。SIRT6 activator 12对SIRT1的IC50值为171.20μM，而对SIRT2、SIRT3、SIRT5的IC50值均大于200μM。SIRT6 activator 12具有显著的抗癌活性，可以用于癌症相关的研究[1-2]。
在体外，SIRT6 activator 12q（2.5-10μM）处理 PANC-1、BXPC-3、MIAPaCa-2 及 AsPC-1等人胰腺导管腺癌（PDAC）细胞系24-72小时。SIRT6 activator 12q显著抑制细胞增殖与迁移，且具有浓度梯度。SIRT6 activator 12q可诱导G2期细胞周期停滞和细胞凋亡，降低组蛋白H3K9、H3K18和H3K56的乙酰化水平，并下调Lin28b和IGF2BP3的表达[1]。
在体内，SIRT6 activator 12q（10mg/kg/day）口服给药，用于处理植入PANC-1细胞异种移植瘤的裸鼠，持续28天。SIRT6 activator 12q显著抑制了肿瘤生长，诱导了肿瘤细胞凋亡，并降低了肿瘤组织中Lin28b的表达[1]。