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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-TCIP3
TCIP3

Chemical Structure : TCIP3

CAS No.: 3067681-36-8

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TCIP3 (KAT-TCIP)

货号: PC-27203Not For Human Use, Lab Use Only.

TCIP3 is a cell-permeable lysine acetyltransferase TCIP (KAT-TCIP) and bivalent molecular glue degrader that binds dually to p300/CBP and BCL6, redirects p300/CBP to BCL6, exhibits potent anti-proliferative effect in DLBCL cells.

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

    生物&药学活性

    TCIP3 is a cell-permeable lysine acetyltransferase TCIP (KAT-TCIP) and bivalent molecular glue degrader that binds dually to p300/CBP and BCL6, redirects p300/CBP to BCL6, exhibits potent anti-proliferative effect in DLBCL cells.
    TCIP3 inhibits the proliferation of SUDHL5 DLBCL cells with an average IC50 of 0.8 nM.
    TCIP3 inhibits the viability of high-BCL6 lines SUDHL5, K422, DB, and DAUDI at comparable potencies (1.2 nM, 4.0 nM, 9.8 nM, and 6.9 nM, respectively), approximately 200 to 1000 times greater than the co-treatment of the inhibitors GNE-781 and BI-3812.
    TCIP3 shows dual engagement with p300/CBP and BCL6.
    TCIP3 induces redirection of p300/CBP acetyltransferase activity to BCL6-proximal DNA.
    TCIP3 acts as a molecular glue, stabilizing interactions between p300/CBP and BCL6.

    物理化学性质&存储条件

    分子量 1177.76
    分子式 C58H71ClF2N16O7
    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

    5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 1-[1-[3-[4-[[1-[5-chloro-4-[[1,2-dihydro-8-methoxy-1-methyl-3-[2-(methylamino)-2-oxoethoxy]-2-oxo-6-quinolinyl]amino]-2-pyrimidinyl]-4-piperidinyl]carbonyl]-1-piperazinyl]-1-oxopropyl]-4-piperidinyl]-3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1,4,6,7-tetrahydro-N-methyl-

    参考文献

    1. Meredith N Nix, et al. bioRxiv [Preprint]. 2025 Mar 17:2025.03.14.643404.

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