基本信息
产品编号:I10297 |
|||||
产品名称:IOX1 |
|||||
CAS: |
5852-78-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
六个月 |
||
分子量: |
189.17 |
-20℃ |
一个月 |
||
化学名: |
|
||||
Solubility (25°C) |
体外 |
DMSO |
37mg/mL (195.59mM) |
||
Ethanol |
Insoluble |
||||
Water |
Insoluble |
||||
体内(现配现用) |
|
|
|||
<1mg/ml表示微溶或不溶。 |
|||||
普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
|||||
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
5.2863mL |
26.4313mL |
52.8625mL |
5mM |
1.0573mL |
5.2863mL |
10.5725mL |
10mM |
0.5286mL |
2.6431mL |
5.2863mL |
50mM |
0.1057mL |
0.5286mL |
1.0573mL |
生物活性
产品描述 |
一种2OG 氧合酶 (2OG oxygenases) 的有效广谱抑制剂,包括 JmjC 去甲基酶。IOX1 抑制 KDM4C,KDM4E,KDM2A,KDM3A 和 KDM6B 的 IC50 值分别为 0.6μM,2.3μM,1.8μM,0.1μM 和 1.4μM。IOX1 抑制 ALKBH5。 |
|||||
靶点/IC50 |
KDM3A |
KDM4C |
KDM6B |
KDM2A |
KDM4E |
|
0.1μM |
0.6μM |
1.6μM |
1.8μM |
2.3μM |
||
体外研究 |
IOX1 (0-200µM;2 hours) inhibits the proliferation and migration of vascular smooth muscle cells (VSMCs) stimulated with angiotensin II (Ang II) in a concentration-dependent manner.IOX1 (200µM;24 hours) blocks the cell cycle progression of angiotensin II (Ang II)-VSMCs by increasing the percentage of cells in the G0/G1 phase.IOX1 (50-200µM;2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in a concentration-dependent.IOX1 (50-200µM;2 hours) mediates cyclin D1 and p21 expression by regaining H3K9me3. Cell Proliferation Assay |
|||||
Cell Line: |
Vascular smooth muscle cells (VSMCs) |
|||||
Concentration: |
50μM,100μM,200μM |
|||||
Incubation Time: |
Pretreated 2 hours |
|||||
Result: |
Exhibited a decrease in proliferation and migration. |
|||||
Cell Cycle Analysis |
||||||
Cell Line: |
Vascular smooth muscle cells (VSMCs) |
|||||
Concentration: |
200μM |
|||||
Incubation Time: |
24 hours |
|||||
Result: |
Slowed down the progression of the cell cycle from the G0/G1 to the S phase. |
|||||
RT-PCR |
||||||
Cell Line: |
Vascular smooth muscle cells (VSMCs) |
|||||
Concentration: |
50μM,100μM,200μM |
|||||
Incubation Time: |
2 hours |
|||||
Result: |
Decreased cyclin D1 mRNA expression and increased p21 mRNA expression. |
|||||
RT-PCR[2] |
||||||
Cell Line: |
Vascular smooth muscle cells (VSMCs) |
|||||
Concentration: |
50μM,100μM,200μM |
|||||
Incubation Time: |
2 hours |
|||||
Result: |
Enhanced the total protein levels of H3K9me3. |
|||||
体内研究 |
IOX1 (5-c-8HQ) (oral gavage;10-20mg/kg;12 days) inhibits tumor growth and attenuates the self-renewal of liver cancer stem-like cells (LCSCs) in vivo. |
|||||
Animal Model: |
Six-week-old male BALB/c nude mice |
|||||
Dosage: |
10mg/kg,20mg/kg |
|||||
Administration: |
12 days |
|||||
Result: |
Did not result in obvious adverse effects on mice as demonstrated by no body weight reduction and no toxicity to the major organs after treatment.Inhibited LCSC orthotopic graft tumor growth.Significantly reduced the protein levels of EpCAM and Sox9 in LCSC orthotopic graft tumors nhibited LCSC orthotopic graft tumor growth.Decreased Ki67-positive tumor cells and markedly reduced the tumorsphere formation abilities of LCSCs in a dose-dependent manner. |
推荐实验方法(仅供参考)
激酶实验: |
|
AlphaScreen 试验 |
所有试剂在50mM HEPES,0.1% BSA,pH 7.5的溶液中稀释,用0.01% Tween20进行增补,在加入到板中之前,使其与室温平衡。催化转换试验在10微升体积的低容量384孔板于室温下进行。反应由酶(5nM),生物素化的底物肽(30nM),Fe(II) (1μM),抗坏血酸盐(100μM),和2OG (10μM)组成,并在室温下进行。对于PHD2,反应由酶(5nM),生物素化的底物肽(60nM),Fe(II) (20μM),抗坏血酸盐(200μM),和2OG (2μM)组成,并在室温下进行。使用EDTA淬灭反应(5微升),加入与多肽抗体(5微升)预培养的AlphaScreen 给体 (链霉亲和素共轭的) 和受体 (蛋白质A共轭的)珠子。将板用箔密封避光保护,在室温下培育60分钟,使用AlphaScreen 680 激发/570发射滤光器在PHERAstar FS板阅读器上读取数据。最终20微升反应液中珠子的浓度为20微克/毫升。与对应的DMSO对照组进行标准化后,IC50值在Prism 6中计算。 |
细胞实验: |
|
细胞系 |
HeLa 细胞 |
浓度 |
~300μ M |
处理时间 |
24小时 |
方法 |
化合物的增殖活性通过MTT测定法确定。HeLa细胞接种在96孔板上,在37 °C下培养24小时以达到70%。随后,将培养基替换为含有1-300μM不同浓度测试化合物的1% DMSO 溶液的DMEM培养基。终浓度为0.03-10μM的星状孢菌素用于细胞毒性对照。处理24小时后,培养基用CellTiter 96 水性单溶液试剂取代,并培养4小时。与相应的1% DMSO处理细胞和含1% DMSO培养基(无细胞)对照组进行标准化后,CC50值在Prism 6软件上计算。 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )