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

BRD7389 

Cat. No.: HY-12185
Handling Instructions

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.

For research use only. We do not sell to patients.

BRD7389 Chemical Structure

BRD7389 Chemical Structure

CAS No. : 376382-11-5

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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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.

376382-11-5

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

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BRD7389BRD 7389BRD-7389Ribosomal S6 Kinase (RSK)S6KRSKSNU-407coloncancerpancreaticisletsdiabetesInhibitorinhibitorinhibit

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