SIRT6 activator 12q是一种SIRT6选择性激活剂（IC50=0.58μM）。
Cas No.:2601734-99-8
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells (human pancreatic ductal adenocarcinoma cell lines) |
Preparation Method | Cells were cultured in Dulbecco's modified Eagle's medium or RPMI1640 supplemented with 10% fetal bovine serum, 100units/mL penicillin, and streptomycin, and grown in a 37°C incubator with a humidified 5% CO₂ atmosphere. Cells were treated with the indicated concentrations of SIRT6 activator 12q (2.5-10μM). |
Reaction Conditions | 2.5-10μM; 24-72h. |
Applications | SIRT6 activator 12q significantly inhibited the proliferation and migration of PDAC cells. SIRT6 activator 12q caused a dose-dependent increase in the percentages of cells in the G2 phase and apoptosis. SIRT6 activator 12q decreased the levels of H3K9ac, H3K18ac, and H3K56ac, and downregulated the expression of Lin28b and IGF2BP3 in the cells. |
| Animal experiment [1]: | |
Animal models | Nude mice bearing PANC-1 cell xenograft tumors |
Preparation Method | Mice were orally administered SIRT6 activator 12q once daily for 28 consecutive days. |
Dosage form | 10mg/kg/day; p.o.; 28 days. |
Applications | SIRT6 activator 12q significantly inhibited tumor growth, induced tumor cell apoptosis, and downregulated the expression of Lin28b in tumor tissues. |
References: | |
| Cas No. | 2601734-99-8 | SDF | Download SDF |
| 分子式 | C31H22N2O2 | 分子量 | 454.52 |
| 溶解度 | DMSO : 25 mg/mL (55.00 mM; ultrasonic and warming and heat to 70°C) | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2001 mL | 11.0006 mL | 22.0012 mL |
| 5 mM | 440 μL | 2.2001 mL | 4.4002 mL |
| 10 mM | 220 μL | 1.1001 mL | 2.2001 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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