For research use only. Not for therapeutic Use.
BET bromodomain inhibitor; blocks recruitment of BET to chromatin. Induces apoptosis and G<sub>0</sub>/G<sub>1</sub> cell cycle arrest in MLL-fusion leukemic cell lines <em>in vitro</em> (IC<sub>50</sub> values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively); reduces BCL2 expression in NOMO1 cells. Improves survival in two rodent models of MLL-fusion leukemia <em>in vivo</em>. Enhances differentiation of human iPSC into megakaryocytes.
| Catalog Number | I010997 |
| CAS Number | 1883545-47-8 |
| Synonyms | 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride |
| Molecular Formula | C23H23Cl2N5O3 |
| Purity | ≥95% |
| Target | Epigenetic Reader Domain |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol and to 100 mM in water |
| Storage | Store at -20C |
| IUPAC Name | 7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one;dihydrochloride |
| InChI | InChI=1S/C23H21N5O3.2ClH/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17;;/h5-11,13H,1-4H3,(H,26,29);2*1H/t13-;;/m1../s1 |
| InChIKey | UFLKDZBLUNJNJS-FFXKMJQXSA-N |
| SMILES | CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC.Cl.Cl |
