For research use only. Not for therapeutic Use.
PLX51107 (CAT: I014575) is a potent and selective inhibitor of the bromodomain-containing protein 4 (BRD4), belonging to the class of BET (bromodomain and extra-terminal) inhibitors. It exhibits novel pharmacologic properties both in vitro and in vivo, surpassing the efficacy of BCR (B-cell receptor) signaling agents in preclinical models of chronic lymphocytic leukemia (CLL). PLX51107 functions by binding to the acetylated lysine recognition motifs within the bromodomains of BRD4. This interaction disrupts the binding of BRD4 to acetylated lysines on histones, thereby impeding chromatin remodeling and gene expression. By modulating these processes, PLX51107 shows promise as a potential therapeutic option for CLL and other diseases where BRD4 plays a critical role.
| Catalog Number | I014575 |
| CAS Number | 1627929-55-8 |
| Synonyms | PLX51107; PLX-51107; PLX 51107.;(S)-4-(6-(3,5-dimethylisoxazol-4-yl)-1-(1-(pyridin-2-yl)ethyl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid |
| Molecular Formula | C26H22N4O3 |
| Purity | ≥95% |
| Target | Epigenetic Reader Domain |
| Solubility | Soluble in DMSO |
| InChI | InChI=1S/C26H22N4O3/c1-15-24(17(3)33-29-15)20-12-23-25(28-13-20)21(18-7-9-19(10-8-18)26(31)32)14-30(23)16(2)22-6-4-5-11-27-22/h4-14,16H,1-3H3,(H,31,32)/t16-/m0/s1 |
| InChIKey | AMSUHYUVOVCWTP-INIZCTEOSA-N |
| SMILES | O=C(O)C1=CC=C(C2=CN([C@H](C3=NC=CC=C3)C)C4=CC(C5=C(C)ON=C5C)=CN=C42)C=C1 |
| Reference | </br>1: Ozer HG, El-Gamal D, Powell B, Hing ZA, Blachly JS, Harrington B, Mitchell S, </br> Grieselhuber NR, Williams K, Lai TH, Alinari L, Baiocchi RA, Brinton L, Baskin E,</br> Cannon M, Beaver L, Goettl VM, Lucas DM, Woyach JA, Sampath D, Lehman AM, Yu L,</br> Zhang J, Ma Y, Zhang Y, Spevak W, Shi S, Severson P, Shellooe R, Carias H, Tsang </br> G, Dong K, Ewing T, Marimuthu A, Tantoy C, Walters J, Sanftner L, Rezaei H, Nespi</br> M, Matusow B, Habets G, Ibrahim P, Zhang C, Mathé EA, Bollag G, Byrd JC,</br> Lapalombella R. BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia</br> Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally</br> Distinct BET Inhibitor. Cancer Discov. 2018 Apr;8(4):458-477. doi:</br> 10.1158/2159-8290.CD-17-0902. Epub 2018 Jan 31. PubMed PMID: 29386193; PubMed</br> Central PMCID: PMC5882533.</br> </br> |
