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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-PITCOIN3
PITCOIN3

Chemical Structure : PITCOIN3

CAS No.: 2397679-88-6

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PITCOIN3 (HB-05-160)

货号: PC-49341Not For Human Use, Lab Use Only.

PITCOIN3 is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.

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

    生物&药学活性

    PITCOIN3 (HB-05-160) is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.
    PITCOIN3 displays high selectivity over other PI3Ks and to PI3K-like protein kinases such as mTOR.
    PITCOIN3 impair PI(3,4)P2 synthesis and endocytosis in HeLa cells, dose-dependently blocks plasma membrane tubule formation induced by constitutively active enhanced green fluorescent protein (eGFP)-SNX9 with EC50 of 4.6 uM.
    PITCOIN3 is nontoxic for in a variety of different cell types, for example, Cos7, HEK293 and HepG2 cells, also has no effect on the Golgi pool of PI(4)P, which is mainly synthesized by PI 4 kinase IIIβ.
    Pharmacological blockade of PI3KC2α by PITCOIN3 (20 uM for 6 h) reduces endosomal PI(3)P levels in Cos7 cells.|
    PITCOIN3 (20 uM for 6 h) impairs platelet membrane remodeling and thrombus formation in mouse resting platelets, causes a pronounced and highly significant reduction in the prothrombotic capacity of platelets, displays antithrombotic activity in mouse blood.

    物理化学性质&存储条件

    分子量 593.695
    分子式 C26H23N7O4S3
    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-(3-(methylsulfonamido)phenyl)thiazol-2-yl)-2-((4-oxo-3-phenethyl-3,4-dihydropteridin-2-yl)thio)acetamide

    参考文献

    1. Lo WT, et al. Nat Chem Biol. 2022 Sep 15. doi: 10.1038/s41589-022-01118-z.
    2. Patent WO2019234237 A1.

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