For research use only. Not for therapeutic Use.
PF-5006739（Cat No.:I011989）is a selective BET (bromodomain and extra-terminal) protein inhibitor, specifically targeting BRD4. It blocks the interaction between BET proteins and acetylated histones, disrupting transcriptional activity in cancer and inflammatory processes. PF-5006739 has been studied for its potential in cancer treatment, particularly in tumors where BET proteins are critical for the expression of oncogenes. By inhibiting BRD4, it reduces tumor growth and proliferation. Its specificity for BET proteins offers a promising approach in developing targeted therapies for cancer and other diseases driven by aberrant gene expression.
| Catalog Number | I011989 |
| CAS Number | 1293395-67-1 |
| Synonyms | PF-5006739; PF 5006739; PF5006739.;4-[4-(4-Fluorophenyl)-1-[1-(3-isoxazolylmethyl)-4-piperidinyl]-1H-imidazol-5-yl]-2-pyrimidinamine |
| Molecular Formula | C22H22FN7O |
| Purity | ≥95% |
| Target | Potent CK1δ/ε inhibitor |
| Solubility | Soluble in DMSO |
| Storage | room temp |
| IUPAC Name | 4-[5-(4-fluorophenyl)-3-[1-(1,2-oxazol-3-ylmethyl)piperidin-4-yl]imidazol-4-yl]pyrimidin-2-amine |
| InChI | InChI=1S/C22H22FN7O/c23-16-3-1-15(2-4-16)20-21(19-5-9-25-22(24)27-19)30(14-26-20)18-6-10-29(11-7-18)13-17-8-12-31-28-17/h1-5,8-9,12,14,18H,6-7,10-11,13H2,(H2,24,25,27) |
| InChIKey | XPWHRQHBPRSUAW-UHFFFAOYSA-N |
| SMILES | C1CN(CCC1N2C=NC(=C2C3=NC(=NC=C3)N)C4=CC=C(C=C4)F)CC5=NOC=C5 |
| Reference | </br>1: Cunningham PS, Ahern SA, Smith LC, da Silva Santos CS, Wager TT, Bechtold DA. </br> Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in</br> obesity. Sci Rep. 2016 Jul 21;6:29983. doi: 10.1038/srep29983. PubMed PMID:</br> 27439882; PubMed Central PMCID: PMC4954991.</br>2: Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler</br> T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G,</br> Sneed B, Walton K, Horton D, Rosado A, Mead A. Casein kinase 1δ/ε inhibitor</br> PF-5006739 attenuates opioid drug-seeking behavior. ACS Chem Neurosci. 2014 Dec</br> 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28. PubMed PMID:</br> 25299732.</br></br> |
