A PRMT1 inhibitor
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TC-E 5003

Item No. 17718

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N'-(sulfonyldi-4,1-phenylene)bis[2-chloro]-acetamide
CAS Number
17328-16-4
Synonyms
  • NSC 30176
Molecular Formula
C16H14Cl2N2O4S
Formula Weight
401.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
257, 283 nm
SMILES
ClCC(NC1=CC=C(S(C2=CC=C(NC(CCl)=O)C=C2)(=O)=O)C=C1)=O
InChi Code
InChI=1S/C16H14Cl2N2O4S/c17-9-15(21)19-11-1-5-13(6-2-11)25(23,24)14-7-3-12(4-8-14)20-16(22)10-18/h1-8H,9-10H2,(H,19,21)(H,20,22)
InChi Key
SHRCVZJKZJGIHQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $49

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    50 mg

    $77

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    100 mg

    $143

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    500 mg

    $423

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    Cayman Chemical
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    Product Description

    TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50 = 1.5 µM for human PRMT1 in a methylation assay).1 It is selective for PRMT1 over PRMT4/CARM1 and SET7/9 methyltransferases, with less than 5% inhibition at a concentration of 50 µM for SET7/9. TC-E 5003 inhibits growth of MCF-7a breast cancer and LNCaP prostate cancer cells (GI50s = 1.97 and 4.49 µM, respectively) and decreases androgen-dependent gene transcription in vitro. TC-E 5003 (80 mg/kg) also has antimalarial properties and eradicates P. berghei in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bissinger, E.M., Heinke, R., Spannhoff, A., et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg. Med. Chem. 19(12), 3717-3731 (2011).

    2. Prescott, B. Potential antimalarial agents. Derivatives of 4,4'-diaminodiphenylsulfone. Int. Z. Klin. Pharmakol. Ther. Toxikol. 4(2), 207-211 (1971).