TDI-011536 是一种有效的Lats激酶抑制剂,能中断Hippo-Yap的信号传导,并可启动受损心肌细胞的增殖。TDI-011536 可用于研究器官的保护和再生。
生物活性 | TDI-011536 is a potentLats kinaseinhibitor, interruptsHippo-Yapsignaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration[1]. |
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体外研究 (In Vitro) | TDI-011536 (3 μM; 24 h) reduces Yap phosphorylation and (3 μM; 5 days) induces proliferation of Müller glia in human retinal organoids[1].
Cell Proliferation Assay[1] Cell Line: | human retinal organoids | Concentration: | 3 μM | Incubation Time: | 24 h, 5 days | Result: | Supressed Yap phosphorylation and promoted Müller glia proliferation. |
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体内研究 (In Vivo) | TDI-011536 (200 mg/kg; i.p.; once) provides over 4 h of Lats inhibition in the liver, heart, and skin and reduces the amount of pYap for at least 4 h after injection in all three organs[1]. TDI-011536 (100 mg/kg; i.p.; once daily for 2 or 3 days) shows proliferative effect on cardiomyocytes[1].
Animal Model: | Living mice (immunoblot analysis of the heart, liver, and skin immediately after injection)[1]. | Dosage: | 200 mg/kg | Administration: | Intraperitoneal injections; once. | Result: | Reduced the amount of pYap for at least 4 h after injection in all three organs and the levels returned to control values within a day. |
Animal Model: | Male 8-week-old mice (cryolesion model)[1]. | Dosage: | 100 mg/kg | Administration: | Intraperitoneal injections; once daily for 2 or 3 days. | Result: | Promoted cardiomyocytes proliferation. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(343.01 mM;Need ultrasonic) 配制储备液 1 mM | 2.7441 mL | 13.7204 mL | 27.4409 mL | 5 mM | 0.5488 mL | 2.7441 mL | 5.4882 mL | 10 mM | 0.2744 mL | 1.3720 mL | 2.7441 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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |