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

中文名称1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
中文同义词化合物 T14779;化合物BRD7389;1-(苯乙基氨基)-2H-萘并[1,2,3-DE]喹啉-2,7(3H)-二酮;BRD-7389,P90核糖体S6激酶RSK抑制剂
英文名称1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
英文同义词BRD 7389;3H-Naphtho[1,2,3-de]quinoline-2,7-dione, 1-[(2-phenylethyl)aMino]-;1-[(2-Phenylethyl)amino]-naphtho-3H-[1,2,3-de]quinoline-2,7-dione;1-Phenethylamino-3H-naphtho[1,2,3-de]quinoline-2,7-dione;1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione;Insulin Expression Inducer, BRD7389;BRD 7389 (BRD7389);Insulin Expression Inducer, BRD7389 - CAS 376382-11-5 - Calbiochem
CAS号376382-11-5
分子式C24H18N2O2
分子量366.41
EINECS号
相关类别
Mol文件376382-11-5.mol
结构式1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione 结构式

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione 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
溶解度二甲基亚砜:>20mg/mL
形态粉末
酸度系数(pKa)11.31±0.40(Predicted)
颜色橙色
稳定性DMSO中的溶液可在-20°下稳定储存3个月。

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione 用途与合成方法

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。

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 )

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.

安全信息

WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-12185BRD73895 mg1000元
2024/04/30HY-121851-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
BRD7389
376382-11-510mg1700元

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione 上下游产品信息

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