BRD0639 is a potent PRMT5 inhibitor. BRD0639 engages the target in cells, disrupts PRMT5-RIOK1 complexes, and reduces substrate methylation. BRD0639 is a first-in-class PBM-competitive inhibitor that can support studies of PBM-dependent PRMT5 activities and the development of novel PRMT5 inhibitors that selectively target these functions.
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| Name | BRD0639 |
|---|---|
| Iupac Chemical Name | (S)-2-(4-chloro-6-oxopyridazin-1(6H)-yl)-N-(4-methyl-3-(N-(2-(pyridin-2-yl)ethyl)sulfamoyl)phenyl)propanamide |
| Synonyms | BRD0639; BRD 0639; BRD-0639; |
| 英文同义词 | BRD0639; BRD 0639; BRD-0639; |
| Molecular Formula | C21H22ClN5O4S |
| Molecular Weight | 475.95 |
| Smile | C[C@H](N1C(C=C(Cl)C=N1)=O)C(NC2=CC=C(C)C(S(=O)(NCCC3=NC=CC=C3)=O)=C2)=O |
| InChiKey | BXDCFRRDENJUJM-HNNXBMFYSA-N |
| 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 |
| CAS Number | 2760881-74-9 |
| 相关CAS号 |
| 包装 | Price | 库存 | Purity | 备货期 |
|---|---|---|---|---|
| 大货 | Enquiry | Enquiry | Enquiry |
| 外观性状 | 固体粉末 |
|---|---|
| Purity | 98% Min. |
| Storage | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
| Solubility | 溶于DMSO |
| 处理方式 | |
| Shipping Condition | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: McKinney DC, McMillan BJ, Ranaghan MJ, Moroco JA, Brousseau M, Mullin- Bernstein Z, O'Keefe M, McCarren P, Mesleh MF, Mulvaney KM, Robinson F, Singh R, Bajrami B, Wagner FF, Hilgraf R, Drysdale MJ, Campbell AJ, Skepner A, Timm DE, Porter D, Kaushik VK, Sellers WR, Ianari A. Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. J Med Chem. 2021 Aug 3. doi: 10.1021/acs.jmedchem.1c00507. Epub ahead of print. PMID: 34342224.