Protein Inhibitors - BI-D1870 (CAS: 501437-28-1)

BI-D1870 (CAS: 501437-28-1)

Catalog #：EBC51067

Biological Activity

Synonyms

RSK inhibitor

Chemical Name

2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridone

Application

BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK)

CAS Number

501437-28-1

Purity

≥99.0%

Molecular Weight

391.40

Molecular Formula

C₁₉H₂₃F₂N₅O₂

SMILES

CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C

Target & IC50

Rsk-1 : IC50 = 31 nM
Rsk-2: IC50 = 24 nM
Rsk-3: IC50 = 18 nM
Rsk-4: IC50 = 15 nM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	2.5549 ml	12.7747 ml	25.5493 ml
5 mM	0.5110 ml	2.5549 ml	5.1099 ml
10 mM	0.2555 ml	1.2775 ml	2.5549 ml
50 mM	0.0511 ml	0.2555 ml	0.5110 ml

Solubility
DMSO: 72 mg/mL (183.9 mM)

Product Description

BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK) (IC50′s at 100μM ATP: Rsk-1 = 31nM, Rsk-2 = 24nM, Rsk-3 = 18nM, Rsk-4 = 15nM). BI-D1870 does not significantly inhibit 10 other AGC kinases, and over 40 other protein kinases at 100X concentrations. BI-D1870 acts on the N-terminal AGC kinase domain and completely prevents PMA-induced TSC2 phosphorylation.