1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione Chemical Properties

Boiling point:

655.0±55.0 °C(Predicted)

Density 

1.35±0.1 g/cm3(Predicted)

storage temp. 

Store at +4°C

solubility 

DMSO: >20mg/mL

form 

powder

pka

11.31±0.40(Predicted)

color 

orange

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Safety Information

WGK Germany 

3

1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione Usage And Synthesis

Description

BRD7389 is an inhibitor of ribosomal S6 kinases (RSKs; IC₅₀s = 1.5, 2.4, and 1.2 μM for RSK1, RSK2, and RSK3, respectively). Through this action, BRD7389 causes mouse αTC1 pancreatic α cells to adopt several morphological and gene expression features of β cells, including increased insulin expression. BRD7389 also enhances glucose-stimulated insulin and glucagon secretion by pancreatic islet cells isolated from human donors with a low body mass index.

Uses

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].

Definition

ChEBI: LSM-4550 is a member of anthracenes.

IC 50

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)

storage

Store at -20°C

References

[1] DINA FOMINA-YADLIN. Small-molecule inducers of insulin expression in pancreatic alpha-cells.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2010: 15099-15104. DOI:10.1073/pnas.1010018107
[2] AMIT CHOUDHARY. Quantitative-proteomic comparison of alpha and Beta cells to uncover novel targets for lineage reprogramming.[J]. PLoS ONE, 2014: e95194. DOI:10.1371/journal.pone.0095194
[3] YANG-SEO PARK  Nam J C. 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.[J]. Molecular and Cellular Biochemistry, 2012, 370 1-2: 191-198. DOI:10.1007/s11010-012-1410-z

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