CONTACT US
Home > Isotope Labeled Compounds>Other Isotope Labeled Compounds> > BI-D1870
BI-D1870

BI-D1870

  • CAT Number: I003762
  • CAS Number: 501437-28-1
  • Molecular Formula: C₁₉H₂₃F₂N₅O₂
  • Molecular Weight: 391.42
  • Purity: ≥95%
Inquiry Now

BI-D1870 (Cat.No:I003762) is a potent and selective inhibitor of the ribosomal S6 kinase (RSK) family, with IC50 values of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4, respectively. It has 10- to 100-fold selectivity for RSK over other protein kinases. BI-D1870 is also a cell-permeable inhibitor that blocks RSK-mediated phosphorylation of downstream targets. Additionally, it has a Kd value of 3.5 μM for the bromodomain-containing protein 4 (BRD4).

Catalog Number I003762
CAS Number 501437-28-1
Molecular Formula

C₁₉H₂₃F₂N₅O₂

Purity 95%
Target S6 Kinase
Solubility DMSO 78 mg/ml; Water <1 mg/ml
Storage 3 years -20℃ powder
IC50 31/24/18/15 nM (for RSK1/RSK2/RSK3/RSK4); 3.5 uM (BRD4) [1] [2]
IUPAC Name 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one
InChI InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
InChIKey DTEKTGDVSARYDS-UHFFFAOYSA-N
SMILES CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
Reference

</br>1:The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Takada I, Yogiashi Y, Makishima M.Immunobiology. 2016 Feb;221(2):188-92. doi: 10.1016/j.imbio.2015.09.008. Epub 2015 Sep 8. PMID: 26386981 </br>2:Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. Roffé M, Lupinacci FC, Soares LC, Hajj GN, Martins VR.Cell Signal. 2015 Aug;27(8):1630-42. doi: 10.1016/j.cellsig.2015.04.004. Epub 2015 Apr 16. PMID: 25889895 </br>3:A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Edgar AJ, Trost M, Watts C, Zaru R.Biosci Rep. 2014 Feb 1;34(1). pii: e00091. Print 2014 Feb 1. PMID: 27919044 Free PMC Article</br>4:A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Edgar AJ, Trost M, Watts C, Zaru R.Biosci Rep. 2013 Dec 17. [Epub ahead of print] PMID: 24341623 </br>5:Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Chiu CF, Bai LY, Kapuriya N, Peng SY, Wu CY, Sargeant AM, Chen MY, Weng JR.Cancer Chemother Pharmacol. 2014 Feb;73(2):237-47. doi: 10.1007/s00280-013-2349-9. Epub 2013 Nov 16. PMID: 24241211 </br>6:The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. Neise D, Sohn D, Stefanski A, Goto H, Inagaki M, Wesselborg S, Budach W, Stühler K, Jänicke RU.Cell Death Dis. 2013 Oct 17;4:e859. doi: 10.1038/cddis.2013.386. PMID: 24136223 Free PMC Article</br>7:BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Sapkota GP, Cummings L, Newell FS, Armstrong C, Bain J, Frodin M, Grauert M, Hoffmann M, Schnapp G, Steegmaier M, Cohen P, Alessi DR.Biochem J. 2007 Jan 1;401(1):29-38. PMID: 17040210 Free PMC Article

Request a Quote

Contact Us at MuseChem

We are committed to providing you with reliable, cost-effective solutions for your chemical needs, while ensuring your safety and comfort. Our team of experts is always available to answer your questions and help you navigate the complexities of the chemical industry.

Whether you're looking for a specific product or need help with a custom synthesis project, we're here to help you discover a new world of chemical possibilities. Contact us today to learn more about how we can assist you with all of your chemical needs.

Our goal is to make the process of ordering chemicals as seamless and hassle-free as possible. Let us know how we can assist you, and we'll get back to you as soon as possible. We look forward to hearing from you!