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BRD7389
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BRD7389图片
CAS NO:376382-11-5
包装与价格:
包装价格(元)
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产品介绍
BRD7389 是一种特异性的RSK家族激酶抑制剂,对RSK1RSK2RSK3IC50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)

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.
分子量

366.41

性状

Solid

Formula

C24H18N2O2

CAS 号

376382-11-5

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7292 mL13.6459 mL27.2918 mL
5 mM0.5458 mL2.7292 mL5.4584 mL
10 mM0.2729 mL1.3646 mL2.7292 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。