Inauhzin
(Synonyms: INZ) 目录号 : GC14755
A selective SIRT1 inhibitor
Cas No.:309271-94-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Inauhzin is a small-molecule inhibitor of SIRT1 with IC50 value of 0.7-2μM [1].
Inauhzin inhibits SIRT1 deacetylation activity and subsequently activates the substrate of SIRT1, p53, in a dose-dependent manner. It shows an induction of acetylation of p53 and Histone H3 in the K382 and K9 residues, respectively. The inhibition of SIRT1 is selective. It has no significant effect on SIRT2, SIRT3 or HDAC8 in the Fluor-de-Lys fluorimetric assay. Since it is an activator of p53, inauhzin inhibits cell growth in different p53-containing human cancer cells including H460, H1299, A549, HT29 and WI38. The IC50 values are 5.4μM, 51.9μM, 3.2μM, 33.9μM and 85.4μM, respectively. Furthermore, inauhzin induces cell apoptosis through activating p53. In the xenograft tumours derived from H460 cells, inauhzin also significantly induces p53 activity and p53-dependent apoptosis at 2μM [1].
References:
[1] Zhang Q, Zeng SX, Zhang Y, Zhang Y, Ding D, Ye Q, Meroueh SO, Lu H. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. EMBO Mol Med. 2012 Apr;4(4):298-312.
| Cell experiment [1]: | |
|
Cell lines |
H460, H1299, A549, HT29 and WI38 |
|
Preparation method |
The solubility of this compound in DMSO is > 23.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
2μM, 18h |
|
Applications |
Inauhzin dose-dependently inhibited cell growth in different p53-containing human cancer cells including H460, H1299, A549, HT29 and WI38. Inauhzin effectively reactivated p53 by inhibiting SIRT1 activity, promoted p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, INZ stabilized p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells. INZ inhibited cell proliferation, induced senescence and tumour-specific apoptosis. |
| Animal experiment [1]: | |
|
Animal models |
Female SCID mice bearing H460 or HCT116 xenografts |
|
Dosage form |
Intraperitoneal injection, 18h, 2μM |
|
Application |
Inauhzin repressed the growth of xenograft tumours derived from p53-harbouring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumour-bearing SCID mice. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Zhang Q, Zeng S X, Zhang Y, et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53[J]. EMBO molecular medicine, 2012, 4(4): 298-312. | |
| Cas No. | 309271-94-1 | SDF | |
| 别名 | INZ | ||
| 化学名 | 2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one | ||
| Canonical SMILES | CCC(SC1=NC2=C(N=N1)C3=CC=CC=C3N2)C(N4C5=CC=CC=C5SC6=CC=CC=C64)=O | ||
| 分子式 | C25H19N5OS2 | 分子量 | 469.58 |
| 溶解度 | ≥ 23.5mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1296 mL | 10.6478 mL | 21.2956 mL |
| 5 mM | 0.4259 mL | 2.1296 mL | 4.2591 mL |
| 10 mM | 0.213 mL | 1.0648 mL | 2.1296 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet