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.
Product information
CAS Number: 376382-11-5
Molecular Weight: 366.41
Formula: C24H18N2O2
Chemical Name: 16-[(2-phenylethyl)amino]-14-azatetracyclo[7.7.1.0, .0, ]heptadeca-1(16), 2, 4, 6, 9(17), 10, 12-heptaene-8, 15-dione
Smiles: O=C1NC2=CC=CC3=C2C(=C1NCCC1C=CC=CC=1)C1=CC=CC=C1C3=O
InChiKey: XASCINRGTHLHGM-UHFFFAOYSA-N
InChi: InChI=1S/C24H18N2O2/c27-23-17-10-5-4-9-16(17)21-20-18(23)11-6-12-19(20)26-24(28)22(21)25-14-13-15-7-2-1-3-8-15/h1-12,25H,13-14H2,(H,26,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line. BRD7389 also increases β-cell-specific gene expression in primary human islet cells. 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.
References:
- 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.
- 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.
Products are for research use only. Not for human use.
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