For research use only. Not for therapeutic Use.
BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML)[1][2].
BRD5648, the inactive enantiomer of BRD0705, does not induce changes in enzyme phosphorylation or total β-catenin protein stabilization[1].
| Catalog Number | I017224 |
| CAS Number | 2056261-42-6 |
| Synonyms | (4R)-4-ethyl-7,7-dimethyl-4-phenyl-1,6,8,9-tetrahydropyrazolo[3,4-b]quinolin-5-one |
| Molecular Formula | C20H23N3O |
| Purity | ≥95% |
| InChI | InChI=1S/C20H23N3O/c1-4-20(13-8-6-5-7-9-13)14-12-21-23-18(14)22-15-10-19(2,3)11-16(24)17(15)20/h5-9,12H,4,10-11H2,1-3H3,(H2,21,22,23)/t20-/m1/s1 |
| InChIKey | NCKLQXXBRWCYMA-HXUWFJFHSA-N |
| SMILES | CCC1(C2=C(NC3=C1C(=O)CC(C3)(C)C)NN=C2)C4=CC=CC=C4 |
| Reference | [1]. Wagner FF, et al. Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. |
