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376382-11-5

中文名稱 1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
英文名稱 1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
CAS 376382-11-5
分子式 C24H18N2O2
分子量 366.41
MOL 文件 376382-11-5.mol
376382-11-5 結構式 376382-11-5 結構式

基本信息

中文別名
化合物BRD7389
化合物 T14779
英文別名
BRD 7389
BRD 7389 (BRD7389)
BRD7389 >=98% (HPLC)
Insulin Expression Inducer, BRD7389
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
1-[(2-Phenylethyl)amino]-naphtho-3H-[1,2,3-de]quinoline-2,7-dione
Insulin Expression Inducer, BRD7389 - CAS 376382-11-5 - Calbiochem
3H-Naphtho[1,2,3-de]quinoline-2,7-dione, 1-[(2-phenylethyl)aMino]-

物理化學性質

沸點655.0±55.0 °C(Predicted)
密度1.35±0.1 g/cm3(Predicted)
儲存條件Store at +4°C
溶解度二甲基亞砜:>20mg/mL
酸度系數(pKa)11.31±0.40(Predicted)
形態(tài)粉末
顏色橙色
穩(wěn)定性DMSO中的溶液可在-20°下穩(wěn)定儲存3個月。

安全數據

危險性描述H413
WGK Germany3

常見問題列表

生物活性
BRD7389 是一種特異性的 RSK 家族激酶抑制劑,對 RSK1,RSK2 和 RSK3 的 IC50 分別為 1.5 μM,2.4 μM 和 1.2 μM。BRD7389 可以誘導胰腺 α 細胞中胰島素表達。
靶點

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 )

體外研究

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.
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