PF-3084014

• CAT Number: I001124
• CAS Number: 1290543-63-3
• Molecular Formula: C27H41F2N5O
• Molecular Weight: 489.64
• Purity: ≥95%
• Target: γ-secretase
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 1.2 nM (whole-cell assay); 6.2 nM (cell-free assay) [1]
• IUPAC Name: (2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-N-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide
• InChI: InChI=1S/C27H41F2N5O/c1-7-8-23(32-20-10-9-18-11-19(28)12-22(29)21(18)13-20)25(35)33-24-14-34(17-31-24)27(5,6)16-30-15-26(2,3)4/h11-12,14,17,20,23,30,32H,7-10,13,15-16H2,1-6H3,(H,33,35)/t20-,23-/m0/s1
• InChIKey: VFCRKLWBYMDAED-REWPJTCUSA-N
• SMILES: CCCC(C(=O)NC1=CN(C=N1)C(C)(C)CNCC(C)(C)C)NC2CCC3=C(C2)C(=CC(=C3)F)F

PF-3084014 (Cat.No:I001124) is a small molecule inhibitor that targets the bromodomain and extra-terminal (BET) family of proteins. It specifically inhibits the interaction between BET proteins and acetylated histones, leading to modulation of gene expression. PF-3084014 has shown potential in preclinical studies as an anti-inflammatory and anti-cancer agent. Further research is ongoing to evaluate its therapeutic applications.

Reference

1:Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014. Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Wood DE, Wood KM, Van Deusen JW, Zhang L.Bioorg Med Chem Lett. 2011 May 1;21(9):2637-40. doi: 10.1016/j.bmcl.2010.12.118. Epub 2010 Dec 30. PMID: 21269827 2:Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. Lanz TA, Wood KM, Richter KE, Nolan CE, Becker SL, Pozdnyakov N, Martin BA, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B.J Pharmacol Exp Ther. 2010 Jul;334(1):269-77. doi: 10.1124/jpet.110.167379. Epub 2010 Apr 2. PMID: 20363853 Free Article