A DMNT1 inhibitor
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GSK3484862

Item No. 38897

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αR-[[3,5-dicyano-6-(dimethylamino)-4-ethyl-2-pyridinyl]thio]-benzeneacetamide
CAS Number
2170136-65-7
Molecular Formula
C19H19N5OS
Formula Weight
365.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
270, 304, 347 nm
SMILES
NC([C@@H](C1=CC=CC=C1)SC2=C(C#N)C(CC)=C(C#N)C(N(C)C)=N2)=O
InChi Code
InChI=1S/C19H19N5OS/c1-4-13-14(10-20)18(24(2)3)23-19(15(13)11-21)26-16(17(22)25)12-8-6-5-7-9-12/h5-9,16H,4H2,1-3H3,(H2,22,25)/t16-/m1/s1
InChi Key
KIEQQZZDWUNUQK-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $61

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    5 mg

    $269

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    10 mg

    $477

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    Cayman Chemical
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    Product Description

    GSK3484862 is an inhibitor of DNA methyltransferase 1 (DNMT1; IC50 = 0.23 µM).1 It is selective for DNMT1 over DNMT3A/3L and DNMT3B/3L (IC50s = >50 µM for both). GSK3484862 (100-1,000 nM) inhibits the growth of MV4-11 leukemia cells. It also decreases promoter DNA methylation in MV4-11 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pappalardi, M.B., Keenan, K., Cockerill, M., et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat. Cancer 2(10), 1002-1017 (2021).