For research use only. Not for therapeutic Use.
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities[1].
BRD0639 is a first-in-class PBM-competitive small molecule that can support studies of PBM dependent PRMT5 activities and the development of novel PRMT5 inhibitors that selectively target these functions. BRD0639 can engage the cellular target and effectively outcompete binding between full-length PRMT5 and RIOK1 proteins with an IC50 of 7.5 uM and 16 uM in permeabilized and living cells, respectively. BRD0639 reduces SDMA in the same subset of proteins also affected by genetic perturbation of the PRMT5 binding motif (PBM) binding site[1].
| Catalog Number | I045379 |
| CAS Number | 2760881-74-9 |
| Synonyms | (2S)-2-(4-chloro-6-oxopyridazin-1-yl)-N-[4-methyl-3-(2-pyridin-2-ylethylsulfamoyl)phenyl]propanamide |
| Molecular Formula | C21H22ClN5O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H22ClN5O4S/c1-14-6-7-18(26-21(29)15(2)27-20(28)11-16(22)13-24-27)12-19(14)32(30,31)25-10-8-17-5-3-4-9-23-17/h3-7,9,11-13,15,25H,8,10H2,1-2H3,(H,26,29)/t15-/m0/s1 |
| InChIKey | BXDCFRRDENJUJM-HNNXBMFYSA-N |
| SMILES | CC1=C(C=C(C=C1)NC(=O)C(C)N2C(=O)C=C(C=N2)Cl)S(=O)(=O)NCCC3=CC=CC=N3 |
| Reference | [1]. McKinney DC, et al. Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. J Med Chem. 2021;64(15):11148-11168. |
