| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H18N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
BRD7389 is a specific inhibitor of the RSK family of kinases, with IC50 values of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. It also acts as a small-molecule inducer of insulin expression in pancreatic α-cells[1]. It is supplied as a light yellow to yellow solid (C24H18N2O2, MW 366.41) at 99.06% purity.
Physical & Chemical Properties
| CAS Number | 376382-11-5 |
|---|---|
| Molecular Formula | C24H18N2O2 |
| Molecular Weight | 366.41 g/mol |
| Purity | 99.06% |
| 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 |
| Target | RSK1, RSK2, RSK3, CDK5/p35, DRAK1, FLT3, PIM1, PKG1α, SGK |
| Signaling Pathway | MAPK/ERK Pathway |
| Solubility | In Vitro: DMSO: 20.83 mg/mL (56.85 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
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) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 20.83 mg/mL (56.85 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
BRD7389 (0.425-6.8 μM) raises insulin expression in mouse α-cells following 3 days of treatment. Insulin (Ins2) mRNA is up-regulated in a dose-dependent manner by BRD7389, peaking at 0.85 μM; treatment for 5 days gives greater induction of insulin gene expression, about 50-fold at 0.85 μM[1]. In a mouse α-cell line, BRD7389 (0.85-6.8μM) significantly raises Pdx1 mRNA expression[1]. In primary human islet cells, BRD7389 also boosts β-cell-specific gene expression[1]. BRD7389 (1 μM; added 30 min prior to Carbachol treatment, 48 h) fully abolishes carbachol-stimulated 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Tension of plus-end tracking protein Clip170 confers directionality and aggressiveness during breast cancer migration. Cell Death Dis 2022 Oct 8;13(10):856. PMID: 36209218
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