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ChemicalBook CAS数据库列表 1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione

生物活性靶点体外研究 1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione 试剂级价格

CAS号:376382-11-5
英文名:1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
中文名:1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
CBNumber:CB62518899
分子式:C24H18N2O2
分子量:366.41
MOL File:376382-11-5.mol

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione化学性质

沸点 :655.0±55.0 °C(Predicted)
密度 :1.35±0.1 g/cm3(Predicted)
储存条件 :Store at +4°C
溶解度 :DMSO: >20mg/mL
形态 :powder
酸度系数(pKa) :11.31±0.40(Predicted)
颜色 :orange
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

安全信息

WGK Germany :3

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione性质、用途与生产工艺

生物活性 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。

靶点

RSK1

1.5 μM (IC ₅₀ )

RSK2

2.4 μM (IC ₅₀ )

RSK3

1.2 μM (IC ₅₀ )

CDK5/p35

6.5 μM (IC ₅₀ )

DRAK1

2.8 μM (IC ₅₀ )

FLT3

3.5 μM (IC ₅₀ )

PIM1

3.7 μM (IC ₅₀ )

PKG1α

6.5 μM (IC ₅₀ )

SGK

13.8 μM (IC ₅₀ )

体外研究

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.