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UNC8153

Chemical Structure : UNC8153

CAS No.: 2929304-60-7

UNC8153 (UNC 8153)

Catalog No.: PC-20356Not For Human Use, Lab Use Only.

UNC8153 (UNC 8153) is a selective NSD2-targeted degrader with binding Kd of 24 nM for NSD2, potently and selectively reduces cellular levels of both NSD2 protein (DC50=350 nM) and H3K36me2 chromatin mark.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    UNC8153 (UNC 8153) is a selective NSD2-targeted degrader with binding Kd of 24 nM for NSD2, potently and selectively reduces the cellular levels of both NSD2 protein (DC50=350 nM) and the H3K36me2 chromatin mark.
    UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 through a novel mechanism.
    UNC8153 downregulates pathological phenotypes in multiple myeloma cells including mild antiproliferative effects in MM1.S cells containing an activating point mutation and antiadhesive effects in KMS11 cells harboring the t(4;14) translocation.

    Physicochemical Properties

    M.Wt 583.69
    Formula C33H37N5O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-(4-((4-((6-aminohexyl)carbamoyl)phenyl)carbamoyl)benzyl)-N-cyclopropyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide

    References

    1. Ronan P Hanley, et al. J Am Chem Soc. 2023 Mar 28. doi: 10.1021/jacs.3c01421.

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