BRD7389

SKU:BHB21900526
Research Validated
Overview
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BRD7389 (CAS 376382-11-5) is an inhibitor supplied as a solid. Reported to act on RSK1, RSK2, RSK3. Relevant to MAPK/ERK Pathway research. Molecular formula C24H18N2O2, molecular weight 366.41 g/mol.
Purity 99.06%
CAS Number 376382-11-5
Molecular Weight 366.41 g/mol
Form Solid
Target RSK1, RSK2, RSK3, CDK5/p35 +5 more
Storage 4°C as supplied; in solvent -80°C
Options selector
Catalog no. Size
HY-12185-5MG 5 mg
HY-12185-10MG 10 mg
HY-12185-25MG 25 mg
HY-12185-50MG 50 mg
HY-12185-100MG 100 mg
HY-12185-200MG 200 mg
HY-12185-500MG 500 mg
HY-12185-1MLX10MM 1 mL x 10 mM (in DMSO)
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 mL x 10 mM (in DMSO)
  • Lead time: varies by selected option.
  • 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.
  • Upon receipt: refrigerate at 4°C as soon as possible.
Field Specification
Target RSK1, RSK2, RSK3, CDK5/p35, DRAK1, FLT3, PIM1, PKG1α, SGK
CAS no. 376382-11-5
Applications
  • Functional Assay (In Vitro)
Molecular weight 366.41
Molecular formula C24H18N2O2
Purity 99.06%
SMILES O=C(C(C=CC=C1)=C1C2=C(NCCC3=CC=CC=C3)C(N4)=O)C5=C2C4=CC=C5
Form Solid
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.
Catalog no. (Mfr.) HY-12185
Main SKU BHB21900526
Inhibitors

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.

[1]. Fomina-Yadlin D, et al. Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15099-104.

[2]. Park YS, et al. EGFR and PKC are involved in the activation of ERK1/2 and p90 RSK and the subsequent proliferation of SNU-407 colon cancer cells by muscarinic acetylcholine receptors. Mol Cell Biochem. 2012 Nov;370(1-2):191-8.

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

SolventSolubilityNotes
DMSO20.83 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 LineMouse α-cell line
Concentration0.425, 0.85, 1.7, 3.4, 6.8 μM
Incubation Time3 days and 5 days
ResultUp-regulated expression of Pdx1.

Cell Proliferation Assay[2]

Cell LineSNU-407 colon cancer cell
Concentration1 μM
Incubation TimeAdded 30 min prior to Carbachol treatment (48 h)
ResultAlmost 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.

Q.Why is there no price on some sizes?
A.Availability and lead time for those sizes are confirmed on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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