A dual inhibitor of PRMT5 and PRMT7
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DS-437

Item No. 29476

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5'-S-[2-[[(ethylamino)carbonyl]amino]ethyl]-5'-thio-adenosine
CAS Number
1674364-87-4
Molecular Formula
C15H23N7O4S
Formula Weight
397.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O=C(NCC)NCCSC[C@@H]1[C@@H](O)[C@@H](O)[C@@](N2C3=NC=NC(N)=C3N=C2)([H])O1
InChi Code
InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1
InChi Key
CACMCLIHCDTJHL-IDTAVKCVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $116

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    10 mg

    $207

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    Cayman Chemical
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    Product Description

    DS-437 is a dual inhibitor of protein arginine methyltransferase 5 (PRMT5) and PRMT7 (IC50s = 5.9 and 6 μM, respectively).1 It is selective for PRMT5 and PRMT7 over a panel of 29 additional protein, DNA, and RNA methyltransferases at 50 μM, but also inhibits DNMT3A and DNMT3B (IC50s = 52 and 62 μM, respectively). DS-437 (2.5 and 10 μM) inhibits symmetrical arginine dimethylation of FOXP3 in HEK293T cells, as well as symmetrical arginine dimethylation of p60 and the ribonucleoproteins SmD1/D3 and SmB/B’ in MDA-MB-231 cells in a concentration-dependent manner.1,2 It inhibits the ability of regulatory T cells (Tregs) to suppress effector T cell (Teff) proliferation in vitro in human and murine Treg suppression assays.2 DS-437 (10 mg/kg five times per week) reduces tumor growth in a CT26Her2 murine colon cancer model when administered in combination with the anti-p185erbB2/neu antibody 4D5.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smil, D., Eram, M.S., Li, F., et al. Discovery of a dual PRMT5-PRMT7 inhibitor. ACS Med. Chem. Lett. 6(4), 408-412 (2015).

    2. Nagai, Y., Ji, M.Q., Zhu, F., et al. PRMT5 associates with the FOXP3 homomer and when disabled enhances targeted p185erbB2/neu tumor immunotherapy. Front. Immunol. 10:174, (2019).