A PRMT6 inhibitor
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SGC6870

Item No. 33712

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(5R-bromo-2-thienyl)carbonyl]-5-(3,5-dimethylphenyl)-1,3,4,5-tetrahydro-7-methyl-2H-1,4-benzodiazepin-2-one
CAS Number
2561471-27-8
Molecular Formula
C23H21BrN2O2S
Formula Weight
469.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: SolubleEthanol: Soluble
SMILES
CC1=CC=C2C([C@](C3=CC(C)=CC(C)=C3)([H])N(C(C4=CC=C(Br)S4)=O)CC(N2)=O)=C1
InChi Code
InChI=1S/C23H21BrN2O2S/c1-13-4-5-18-17(11-13)22(16-9-14(2)8-15(3)10-16)26(12-21(27)25-18)23(28)19-6-7-20(24)29-19/h4-11,22H,12H2,1-3H3,(H,25,27)/t22-/m1/s1
InChi Key
NIPTUMFVYBXSMZ-JOCHJYFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $68

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    Product Description

    SGC6870 is an inhibitor of protein arginine methyltransferase 6 (PRMT6; IC50 = 77 nM).1 It is selective for PRMT6 over a panel of 76 methyltransferases, G protein-coupled receptors (GPCRs), ion channels, receptors, and other enzymes at 1 µM. SGC6870 decreases the levels of dimethylated arginine 2 on histone 3 (H3R2me2) and dimethylated arginine 3 on histone 4 (H4R3me2) in HEK293T cells (IC50s = 0.9 and 0.6 µM, respectively). See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shen, Y., Li, F., Szewczyk, M.M., et al. A first-in-class, highly selective and cell-active allosteric inhibitor of protein arginine methyltransferase 6. J. Med. Chem. 64(7), 3697-3706 (2021).