501437-28-1
501437-28-1
Chemical Structure
BI-D1870
- CAS No.: 501437-28-1
- Formula:C19H23F2N5O2
- Molecular Weight:391.42
IUPAC Name: 2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one
InChIKey: DTEKTGDVSARYDS-UHFFFAOYSA-N
SMILES: OC1=C(F)C=C(NC2=NC(N(CCC(C)C)C(C)C(N3C)=O)=C3C=N2)C=C1F
Biological Activity: 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].
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BI-D1870 | 99.43% | 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. | ||||||||||||||||||||
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BI-D1870 (Standard) | ≥98% | BI-D1870 (Standard) is the analytical standard of BI-D1870 (HY-10510). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
