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 |
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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; |
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 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | Solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
HS Code |
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Mechanism | |
Cell study | |
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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.