JGB1741 (ILS-JGB-1741) 是一种有效且特异性的SIRT1活性抑制剂，IC50为 ~15 μM。JGB1741 对 SIRT2 和 SIRT3 具有弱的抑制作用，IC50>100 μM。JGB1741 通过调节 Bax/Bcl2 比率、细胞色素 c 释放和 PARP 裂解来增加乙酰化 p53 水平，导致 p53 介导的细胞凋亡。JGB1741 具有用于乳腺癌研究的潜力。
| 生物活性 | JGB1741 (ILS-JGB-1741) is a potent and specificSIRT1activity inhibitor with anIC50of ~15 μM. JGB1741 is a weakSIRT2andSIRT3 inhibitorwith an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediatedapoptosiswith modulation of Bax/Bcl2 ratio, cytochrome c release andPARPcleavage. JGB1741 has the potential for breastcancerresearch[1]. |
| IC50& Target[1] | SIRT1 ∼15 μM (IC50) | SIRT2 >100 μM (IC50) | SIRT3 >100 μM (IC50) |
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体外研究
(In Vitro) | JGB1741 (ILS-JGB-1741; 1-10000 nM; 24 h) inhibits MDA-MB 231 cell proliferation[1].
JGB1741 (0.01-1 μM; 24 h) induces apoptosis of MDA-MB 231 cells[1].
JGB1741 (0.01-1 μM; 24 h) shows a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase[1].
JGB1741 (0.01-1 μM; 24 h) shows an increase in the global acetylation of H3K9, p53 expression and acetylated p53K382 levels[1].
Cell Proliferation Assay[1] | Cell Line: | K562, HepG2 and MDA-MB 231 cell lines | | Concentration: | 1, 10, 50, 100, 500, 1000, 10000 nM | | Incubation Time: | 24 hours | | Result: | Inhibited MDA-MB 231 cell proliferation more potently with an IC50of 0.5 μM than K562 and HepG2 cell proliferation (IC50>1 μM). |
Apoptosis Analysis[1] | Cell Line: | MDA-MB 231 cells | | Concentration: | 0.01, 0.1, 0.5, 1 μM | | Incubation Time: | | | Result: | Showed an increase in the percent apoptotic cells in a dose-dependent fashion with ~70% apoptosis at 1 μM concentration. |
Cell Cycle Analysis[1] | Cell Line: | MDA-MB 231 cells | | Concentration: | 0.01, 0.1, 0.5, 1 μM | | Incubation Time: | | | Result: | Showed a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase, the apoptotic phase, in a dose-dependent fashion. |
Western Blot Analysis[1] | Cell Line: | MDA-MB 231 cells | | Concentration: | 0.01, 0.1, 0.5, 1 μM | | Incubation Time: | | | Result: | Caused a dose-dependent increase in the global acetylation of H3K9.
Showed an increase in both p53 expression and acetylated p53K382 levels. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(11.35 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2698 mL | 11.3492 mL | 22.6984 mL | | 5 mM | 0.4540 mL | 2.2698 mL | 4.5397 mL | | 10 mM | 0.2270 mL | 1.1349 mL | 2.2698 mL |
*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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
