INY-03-041 是一种有效的、高选择性的、基于 PROTAC 的泛-AKT降解剂，由ATP 竞争性AKT抑制剂Ipatasertib (HY-15186) 结合 Lenalidomide (HY-A0003，Cereblon配体)组成。INY-03-041 可抑制AKT1，AKT2和AKT3，IC50分别为 2.0 nM，6.8 nM 和 3.5 nM。
| 生物活性 | INY-03-041 is a potent, highly selective and PROTAC-based pan-AKTdegrader consisting of the ATP-competitiveAKTinhibitorIpatasertib(HY-15186) conjugated toLenalidomide(HY-A0003,Cereblonligand). INY-03-041 inhibitsAKT1,AKT2andAKT3withIC50s of 2.0, 6.8 and 3.5 nM, respectively[1]. |
| IC50& Target[1] | Akt1 2.0 nM (IC50) | Akt3 3.5 nM (IC50) | Akt2 6.8 nM (IC50) | Cereblon |
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体外研究
(In Vitro) | INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50=37.3 nM) and PKG1 (IC50= 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared withIpatasertib(HY-15186) in MDA-MB-468 and HCC1937 cells[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout[1].
Western Blot Analysis[1] | Cell Line: | MDA-MB-468 cells | | Concentration: | 10 nM, 50 nM, 100 nM, 250 nM, 500 nM, 1000 nM | | Incubation Time: | 2 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours | | Result: | Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 115 mg/mL(144.04 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 1.2525 mL | 6.2624 mL | 12.5249 mL | | 5 mM | 0.2505 mL | 1.2525 mL | 2.5050 mL | | 10 mM | 0.1252 mL | 0.6262 mL | 1.2525 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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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