SIRT7 inhibitor 97491
目录号 : GC60338
SIRT7 inhibitor 97491是一种有效的SIRT 7抑制剂,以剂量依赖性方式降低SIRT7的脱乙酰酶活性,IC50为325 nM。
Cas No.:1807758-81-1
Sample solution is provided at 25 µL, 10mM.
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SIRT7 inhibitor 97491 is a potent SIRT 7 inhibitor that reduces the deacetylase activity of SIRT7 in a dose-dependent manner with an IC50 of 325 nM. SIRT7 inhibitor 97491 increases p53 stability through acetylation at K373/382. In addition, SIRT7 inhibitor 97491 promotes cell apoptosis through the caspase pathway[1].
In vitro, treatment with SIRT7 inhibitor 97491 (5 µM, 10 µM) for 72 hours resulted in a reduction of MES-SA cell proliferation by more than 50% without causing toxic effects on HEK 293 cells[1].
In vivo, three weeks of treatment with SIRT7 inhibitor 97491 (20 mg/kg/day; i.p.) inhibited tumor growth in xenograft mice[1].
References:
[1] Ji-Hye Kim, et al. Identification of a Novel SIRT7 Inhibitor as Anticancer Drug Candidate. Biochem Biophys Res Commun. 2019 Jan 8;508(2):451-457.
SIRT7 inhibitor 97491是一种有效的SIRT 7抑制剂,以剂量依赖性方式降低SIRT7的脱乙酰酶活性,IC50为325 nM。 SIRT7 inhibitor 97491通过在K373/382处乙酰化增加p53稳定性。此外,SIRT7 inhibitor 97491通过caspase途径促进细胞凋亡[1]。
在体外,SIRT7 inhibitor 97491(5µM 、10 µM)浓度处理72h导致MES-SA细胞增殖减少超过了50%,而不会对HEK 293细胞造成毒性影响[1]。
在体内,SIRT7 inhibitor 97491 (20mg/kg/day; i.p.) 治疗三周可以抑制异种移植小鼠的肿瘤生长[1]。
| Cell experiment [1]: | |
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Cell lines |
MES-SA cells |
|
Preparation Method |
cells were seeded at a final concentration of 2 x 104 cells/mL and 3 x 103 cells/mL, respectively, in a 96-well plate. SIRT7 inhibitor 97491 was dissolved in DMSO , and the cells were treated with diverse concentrations (0, 1, 5, and 10 mM) of SIRT7 inhibitor 97491. Cell viability and cell proliferation were determined after 24 and 72 h of incubation, respectively. |
|
Reaction Conditions |
1, 5, 10 µM; 24, 72h |
|
Applications |
SIRT7 inhibitor 97491 lead to more than 50% decrease in cell proliferation at concentrations of 5 and 10 µM. |
| Animal experiment [2]: | |
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Animal models |
Balb/c nude mice |
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Preparation Method |
MES-SA cells (5 x 106 cells) were injected subcutaneously into the right flank of female nude mice. The mice were treated with doxorubicin (2 mg/kg/day) or SIRT7 inhibitor 97491 (20 mg/kg/day) for 3 weeks, except for weekends (n =5 per group). Doxorubicin was used as a general anticancer chemotherapy agent. After 21 days of treatment, the mice were sacrificed and the tumors were harvested. |
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Dosage form |
20mg/kg/day; i.p.；3 weeks |
|
Applications |
SIRT7 inhibitor 97491 exerted a strong anticancer effect, similar to but more specific than doxorubicin, on tumor proliferation in vivo, without causing any side effects. |
|
References: [1] Ji-Hye Kim, et al. Identification of a Novel SIRT7 Inhibitor as Anticancer Drug Candidate. Biochem Biophys Res Commun. 2019 Jan 8;508(2):451-457. | |
| Cas No. | 1807758-81-1 | SDF | |
| Canonical SMILES | NC1=CC(NC2=NC=C(C3=CC=C(Cl)C=C3)O2)=CC=C1 | ||
| 分子式 | C15H12ClN3O | 分子量 | 285.73 |
| 溶解度 | DMSO :57 mg/mL(199.48 mM; Moisture absorption of DMSO will reduce the solubility of the compound, please use newly opened DMSO) | 储存条件 | 4°C, protect from light |
| 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。 |
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| 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 | 3.4998 mL | 17.499 mL | 34.9981 mL |
| 5 mM | 0.7 mL | 3.4998 mL | 6.9996 mL |
| 10 mM | 0.35 mL | 1.7499 mL | 3.4998 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet