For research use only. Not for therapeutic Use.
FX1 (Cat.No:I011908) is an inhibitor of the B cell lymphoma 6 (BCL6). FX1 has 10-fold greater potency than endogenous corepressors and binds an essential region of the BCL6 lateral groove. FX1 disrupted formation of the BCL6 repression complex, reactivated BCL6 target genes, and mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations. Low doses of FX1 induced regression of established tumors in mice bearing DLBCL xenografts. Furthermore, FX1 suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo.
| Catalog Number | I011908 |
| CAS Number | 1426138-42-2 |
| Synonyms | FX1; FX-1; FX 1.;(5Z)-5-(5-Chloro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinepropanoic acid |
| Molecular Formula | C14H9ClN2O4S2 |
| Purity | ≥95% |
| Target | Bcl-2 Family |
| Solubility | Soluble in DMSO |
| Storage | Store at 0-8 °C |
| IUPAC Name | 3-[5-(5-chloro-2-oxoindol-3-yl)-4-hydroxy-2-sulfanylidene-1,3-thiazol-3-yl]propanoic acid |
| InChI | InChI=1S/C14H9ClN2O4S2/c15-6-1-2-8-7(5-6)10(12(20)16-8)11-13(21)17(14(22)23-11)4-3-9(18)19/h1-2,5H,3-4H2,(H,16,20)(H,18,19)/b11-10- |
| InChIKey | VISHSGZPGQKEFX-KHPPLWFESA-N |
| SMILES | O=C(O)CCN(C/1=O)C(SC1=C2C(NC3=C/2C=C(Cl)C=C3)=O)=S |
| Reference | </br>1: Cardenas MG, Yu W, Beguelin W, Teater MR, Geng H, Goldstein RL, Oswald E,</br> Hatzi K, Yang SN, Cohen J, Shaknovich R, Vanommeslaeghe K, Cheng H, Liang D, Cho </br> HJ, Abbott J, Tam W, Du W, Leonard JP, Elemento O, Cerchietti L, Cierpicki T, Xue</br> F, MacKerell AD Jr, Melnick AM. Rationally designed BCL6 inhibitors target</br> activated B cell diffuse large B cell lymphoma. J Clin Invest. 2016 Sep</br> 1;126(9):3351-62. doi: 10.1172/JCI85795. Epub 2016 Aug 2. PubMed PMID: 27482887; </br> PubMed Central PMCID: PMC5004937.</br></br> |
