BI-D1870 - 5 mg

Activity: p90 Ribosomal S6 kinase inhibitor . Function/Pharmacology: BI-D1870 is an inhibitor of p90 ribosomal S6 kinase (RSK; IC50’s = RSK1, 31 nM; RSK2, 24 nM; RSK3, 18 nM; RSK4, 15 nM) with selectivity over other AGC kinases.1 It protected mice from experimental autoimmune encephalomyelitis suggesting a new strategy to treat multiple sclerosis.2 BI-D1870 has also been found to alter mTORC1 signaling in an RSK-independent manner.3 BI-D1870 induced apoptosis in oral squamous cell carcinoma cells4, suppressed growth and induced apoptosis in pediatric medulloblastoma cell lines as well as sensitizing these lines to Sonic hedgehog agents5, and blocked cell proliferation and protein synthesis in dual BRAF and MEK inhibitor-resistant melanoma6. Chemical Name: 2-(3,5-Difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one