BI-D1870
BI-D1870 is a potent and specific RSK inhibitor (the p90 ribosomal S6 kinase), which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10–30 nM. BI-D1870 exhibited a dose-responsive antiproliferative effect on OSCC cells with relative sparing of normal human oral keratinocytes. The compound inhibited the downstream RSK target YB-1 and caused apoptosis. In addition, BI-D1870 also induced G2/M arrest by modulating the expression of p21 and other cell cycle regulators. BI-D1870 may be of useful in oral squamous cell carcinoma therapy.
1: Edgar AJ, Trost M, Watts C, Zaru R. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep. 2013 Dec 17. [Epub ahead of print] PubMed PMID: 24341623; PubMed Central PMCID: PMC3908613.
2: Chiu CF, Bai LY, Kapuriya N, Peng SY, Wu CY, Sargeant AM, Chen MY, Weng JR. Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):237-47. doi: 10.1007/s00280-013-2349-9. Epub 2013 Nov 16. PubMed PMID: 24241211.
3: Neise D, Sohn D, Stefanski A, Goto H, Inagaki M, Wesselborg S, Budach W, Stühler K, Jänicke RU. 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. Cell Death Dis. 2013 Oct 17;4:e859. doi: 10.1038/cddis.2013.386. PubMed PMID: 24136223; PubMed Central PMCID: PMC3920941.
4: Sapkota GP, Cummings L, Newell FS, Armstrong C, Bain J, Frodin M, Grauert M, Hoffmann M, Schnapp G, Steegmaier M, Cohen P, Alessi DR. 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. PubMed PMID: 17040210; PubMed Central PMCID: PMC1698666.
2: Chiu CF, Bai LY, Kapuriya N, Peng SY, Wu CY, Sargeant AM, Chen MY, Weng JR. Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):237-47. doi: 10.1007/s00280-013-2349-9. Epub 2013 Nov 16. PubMed PMID: 24241211.
3: Neise D, Sohn D, Stefanski A, Goto H, Inagaki M, Wesselborg S, Budach W, Stühler K, Jänicke RU. 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. Cell Death Dis. 2013 Oct 17;4:e859. doi: 10.1038/cddis.2013.386. PubMed PMID: 24136223; PubMed Central PMCID: PMC3920941.
4: Sapkota GP, Cummings L, Newell FS, Armstrong C, Bain J, Frodin M, Grauert M, Hoffmann M, Schnapp G, Steegmaier M, Cohen P, Alessi DR. 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. PubMed PMID: 17040210; PubMed Central PMCID: PMC1698666.
| Chemical | |
|---|---|
| CAS Num | 501437-28-1 |
| Chemical Formula | C19H23F2N5O2 |
| Molecular Weight | 391.41 |
| IUPAC Chemical Name | 2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one. |
| Exact Mass | 391.18198 |
| Elemental Analysis | C, 58.30; H, 5.92; F, 9.71; N, 17.89; O, 8.18 |
| Synonym | BID1870; BI D1870; BI-D1870. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C1N(C)C2=CN=C(NC3=CC(F)=C(O)C(F)=C3)N=C2N(CCC(C)C)C1C |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Pale orange to brown solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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