BRD7389

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BRD7389 是 RSK 家族激酶的抑制剂，对 RSK1、RSK2 和 RSK3 的 IC50 值分别为 1.5 μM、2.4 μM 和 1.2 μM。

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.(In Vitro):BRD7389 (1 μM) almost completely blocked Carbachol (1 mM)-stimulated cell proliferation, but has little effect on the basal level of proliferation. BRD7389 (0.425, 0.85, 1.7, 3.4, 6.8 μM) induces insulin expression in mouse α-cells and induces a dose-dependent up-regulation of insulin (Ins2) mRNA, peaking at 0.85 μM. BRD7389 increases β-cell-specific gene expression in primary human islet cells. BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line.

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.BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line.BRD7389 also increases β-cell-specific gene expression in primary human islet cells. 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. RT-PCR 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 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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Others

Other Targets

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376382-11-5

366.42

C24H18N2O2

>98% (HPLC)

In Vitro:?DMSO : 20.83 mg/mL (56.85 mM)

O=C1c2ccccc2-c2c(NCCc3ccccc3)c(=O)[nH]c3cccc1c23

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(-20℃)

With Ice Pack

≥ 2 years