2. MAPK/ERK Pathway
  3. Ribosomal S6 Kinase (RSK)
  4. BRD7389

BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.

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BRD7389 Chemical Structure

BRD7389 Chemical Structure

CAS No. : 376382-11-5

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Based on 1 publication(s) in Google Scholar

BRD7389 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BRD7389

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Description

BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression 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)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BRD7389 Related Antibodies

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.
Molecular Weight

366.41

Formula

C24H18N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(C=CC=C1)=C1C2=C(NCCC3=CC=CC=C3)C(N4)=O)C5=C2C4=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (56.85 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7292 mL 13.6459 mL 27.2918 mL
5 mM 0.5458 mL 2.7292 mL 5.4584 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.75%

COA (251 KB) HNMR (237 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7292 mL 13.6459 mL 27.2918 mL 68.2296 mL
5 mM 0.5458 mL 2.7292 mL 5.4584 mL 13.6459 mL
10 mM 0.2729 mL 1.3646 mL 2.7292 mL 6.8230 mL
15 mM 0.1819 mL 0.9097 mL 1.8195 mL 4.5486 mL
20 mM 0.1365 mL 0.6823 mL 1.3646 mL 3.4115 mL
25 mM 0.1092 mL 0.5458 mL 1.0917 mL 2.7292 mL
30 mM 0.0910 mL 0.4549 mL 0.9097 mL 2.2743 mL
40 mM 0.0682 mL 0.3411 mL 0.6823 mL 1.7057 mL
50 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3646 mL
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BRD7389 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD7389376382-11-5BRD 7389BRD-7389Ribosomal S6 Kinase (RSK)S6KRSKSNU-407coloncancerpancreaticisletsdiabetesInhibitorinhibitorinhibit

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