BRD7389 是一种特异性的RSK家族激酶抑制剂，对RSK1，RSK2和RSK3的IC50分别为 1.5 μM，2.4 μM 和 1.2 μM。BRD7389 可以诱导胰腺 α 细胞中胰岛素表达。
| 生物活性 | BRD7389 is a specificRSKfamily kinase inhibitor withIC50s of 1.5 μM, 2.4 μM, and 1.2 μM forRSK1,RSK2, andRSK3, respectively. BRD7389 is a small-molecule inducer ofinsulinexpression in pancreatic α-cells[1]. |
| IC50& Target[1] | RSK1 1.5 μM (IC50) | RSK2 2.4 μM (IC50) | RSK3 1.2 μM (IC50) | CDK5/p35 6.5 μM (IC50) | DRAK1 2.8 μM (IC50) | FLT3 3.5 μM (IC50) | PIM1 3.7 μM (IC50) | PKG1α 6.5 μM (IC50) | SGK 13.8 μM (IC50) |
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体外研究
(In Vitro) | BRD7389 (0.425-6.8 μM) induces insulin expression in mouse α-cells after 3 days treatment. BRD7389 induces a dose-dependent up-regulation of insulin (Ins2) mRNA, peaking at 0.85 μM; 5 days treatment with BRD7389 results in greater induction of insulin gene expression, about 50-fold at 0.85 μM[1].
BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line[1].
BRD7389 also increases β-cell-specific gene expression in primary human islet cells[1].
BRD7389 (1 μM; added 30 min prior to Carbachol treatment 48 h) fully abolishes carbachols timulated cell proliferation, but has little effect on the basal level of proliferation[2].
RT-PCR[1] | Cell Line: | Mouse α-cell line | | Concentration: | 0.425, 0.85, 1.7, 3.4, 6.8 μM | | Incubation Time: | 3 days and 5 days | | Result: | Up-regulated expression of Pdx1. |
Cell Proliferation Assay[2] | Cell Line: | SNU-407 colon cancer cell | | Concentration: | 1 μM | | Incubation Time: | Added 30 min prior to Carbachol treatment (48 h) | | Result: | Almost completely blocked Carbachol (1 mM)-stimulated cell proliferation. |
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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 : 20.83 mg/mL(56.85 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.7292 mL | 13.6459 mL | 27.2918 mL | | 5 mM | 0.5458 mL | 2.7292 mL | 5.4584 mL | | 10 mM | 0.2729 mL | 1.3646 mL | 2.7292 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。 |
