An inhibitor of the protein-peptide interaction between PRMT5 and PBM
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BRD0639

Item No. 35625

Technical Information
Formal Name
(αS)-4-chloro-α-methyl-N-[4-methyl-3-[[[2-(2-pyridinyl)ethyl]amino]sulfonyl]phenyl]-6-oxo-1(6H)-pyridazineacetamide
CAS Number
2760881-74-9
Molecular Formula
C21H22ClN5O4S
Formula Weight
Purity
≥98%
A solid
DMF: 5 mg/mlDMSO: 5 mg/mlEthanol: 5 mg/ml
λmax
211, 252 nm
SMILES
ClC(C=NN1[C@@H](C)C(NC2=CC=C(C)C(S(NCCC3=NC=CC=C3)(=O)=O)=C2)=O)=CC1=O
InChi Code
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
InChi Key
BXDCFRRDENJUJM-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BRD0639 is an inhibitor of the protein-peptide interaction between protein arginine methyltransferase 5 (PRMT5) and PRMT5 binding motif (PBM; IC50 = 13.8 µM), a conserved peptide motif contained in PRMT5 substrate adaptor proteins (SAPs) that mediates SAP binding to PRMT5.1 It induces the formation of PRMT5 adducts in cells (EC50 = 3 µM) and disrupts complex formation between PRMT5 and the SAP RIO kinase 1 (RIOK1) in permeabilized cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McKinney, D.C., McMillan, B.J., Ranaghan, M.J., et alDiscovery of a first-in-class inhibitor of the PRMT5−substrate adaptor interaction. J. Med. Chem. 64(15), 11148-11168 (2022).