AMPK-IN-3 (化合物 67) 是一种强效的、选择性的AMPK抑制剂，其对AMPK (α2)、AMPK (α1)和KDR的IC50值分别为 60.7、107 和 3820 nM。AMPK-IN-3 对AMPK的抑制不影响细胞活力或导致 K562 细胞的明显细胞毒性。AMPK-IN-3 可用于癌症的研究。
| 生物活性 | AMPK-IN-3 (compound 67) is a potent and selectiveAMPKinhibitor withIC50s of 60.7, 107 and 3820 nM forAMPK(α2),AMPK(α1)andKDR, respectively. AMPK-IN-3 inhibitsAMPKdoes not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study ofcancer[1]. |
| IC50& Target[1] | AMPK (α2) 60.7 nM (IC50) | AMPK (α1) 107 nM (IC50) | KDR 3820 nM (IC50) |
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体外研究
(In Vitro) | AMPK-IN-3 (100 nM) shows inhibition values for AMPK(α2), FLT1, JAK1 JH2-pseudokinase and AMPK(α1) for 64%, 43%, 41% and 29%, respectively[1].
AMPK-IN-3 (0.195313, 0.78125, 3.125, 12.5, 50 μM; 2 h) decreases the level of p-ACC in K562 cells[1].
AMPK-IN-3 (1-100 μM; 24, 48, 72 h) shows potent inhibition of cellular AMPK activity but not affect cell viability[1].
Cell Viability Assay[1] | Cell Line: | K562 cells | | Concentration: | 0.195313, 0.78125, 3.125, 12.5, 50 μM | | Incubation Time: | 2 h | | Result: | Decreased cellular levels of p-ACC(Ser79) in K562 cells. |
Cell Viability Assay[1] | Cell Line: | K562 cells | | Concentration: | 1-100 μM | | Incubation Time: | 24, 48, 72 h | | Result: | Showed no measurable impact on cell viability in K562 cells cultured under hypoxic conditions for 72 hours. |
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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 : 115 mg/mL(254.67 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2145 mL | 11.0727 mL | 22.1455 mL | | 5 mM | 0.4429 mL | 2.2145 mL | 4.4291 mL | | 10 mM | 0.2215 mL | 1.1073 mL | 2.2145 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。 |
