BI-D1870

BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively[1][2][3][4][5].

Product Specifications

CAS Number

[501437-28-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Ribosomal S6 Kinase (RSK)

Type

Reference compound

Related Pathways

Autophagy; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BI-D1870.html

Purity

99.43

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC1=C(F)C=C(NC2=NC(N(CCC(C)C)C(C)C(N3C)=O)=C3C=N2)C=C1F

Molecular Formula

C19H23F2N5O2

Molecular Weight

391.42

Precautions

H302, H315, H319, H335

References & Citations

[1]Sapkota GP, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401 (1) :29-38.|[2]Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2.|[3]Takada I, et al. The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Immunobiology. 2016 Feb;221 (2) :188-92.|[4]Roffe M, et al. Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. Cell Signal. 2015 Aug;27 (8) :1630-42.|[5]Chiu CF, et al. Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73 (2) :237-47.