Drug intelligence / Profile preview

BI-D1870

Development stage
Preclinical
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
In Vitro, Intravenous (preclinical Animal Studies)
01

Overview

**BI-D1870** is a potent, selective small molecule inhibitor of **ribosomal S6 kinase (RSK)** isoforms—specifically RSK1, RSK2, RSK3, and RSK4—acting as an ATP-competitive inhibitor predominantly at the N-terminal AGC kinase domain[1][7][9]. It displays nanomolar inhibitory potency and has minimal effect on other related kinases, making it a valuable tool for studying RSK biology and as a preclinical investigational agent. BI-D1870 causes G2/M phase cell cycle arrest and induces apoptosis in a range of cancer cell lines—including acute myeloid leukemia (AML) and neuroblastoma—by blocking mitotic exit and interfering with protein translation (partly through inhibition of the PI3K-Akt-mTORC1 signaling pathway)[2][3][4][6][8]. Originally developed by Boehringer Ingelheim, BI-D1870 has been used primarily in preclinical research settings.

Other names
2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridone
02

Targets

RPS6KA3 (RSK2)RPS6KA1 (Ribosomal S6 kinase Alpha-1)RPS6KA4 (Ribosomal protein S6 kinase alpha-4)VRK1 (Vaccinia-related kinase 1)

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