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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-CAS-010
CAS-010

Chemical Structure : CAS-010

CAS No.: 3094094-17-1

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CAS-010 (CAS010, CAS-13312-010)

货号: PC-25366Not For Human Use, Lab Use Only.

CAS-010 (CAS-13312-010) is a potent, selective and ubiquitin-competitive inhibitor of USP28 with IC50 of 4.2 nM in UbRho assays, disrupts the 53BP1-USP28 interaction and reduces p53 target gene transactivation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    CAS-010 (CAS-13312-010) is a potent, selective and ubiquitin-competitive inhibitor of USP28 with IC50 of 4.2 nM in UbRho assays, disrupts the 53BP1-USP28 interaction and reduces p53 target gene transactivation.
    CAS-010 inhibits recombinant full-length (FL) USP28 with single-digit nanomolar potency (IC50=2.2 nM).
    CAS-010 inhibits closely related USP25 with IC50 of 75 nM (USP25 CD) and 51 nM (USP25 FL).
    CAS-010 blocks ABP labeling of USP28 and USP25 in a dose dependent manner in ABPP-MS experiment in HCT116 lysate, but not binding the other 57 DUBs de tected.
    CAS-010 recapitulates the effects of USP28 genetic loss, both with respect to viability and p53 relationship.
    CAS-010 attenuates p53 gene transactivation.
    CAS-010 significantly decreases 53BP1-USP28 PLA foci in both cell lines and conditions in RPE-1 and U2OS cells, both with and without IR-induced DNA damage.

    物理化学性质&存储条件

    分子量 448.63
    分子式 C26H32N4OS
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    N-(4-(8-azabicyclo[3.2.1]octan-3-yl)phenethyl)-3-amino-6-propylthieno[2,3-b]pyridine-2-carboxamide

    参考文献

    1. Bratt AS, et al. Cell Chem Biol. 2025 Sep 1:S2451-9456(25)00232-6.

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