生物活性 靶点 体外研究 871543-07-6 试剂级价格
ChemicalBook  CAS数据库列表  871543-07-6

871543-07-6

871543-07-6,871543-07-6,结构式
871543-07-6
  • CAS号:871543-07-6
  • 英文名:H1152, DIHYDROCHLORIDE
  • 中文名:871543-07-6
  • CBNumber:CB6506731
  • 分子式:C16H21N3O2S
  • 分子量:319.42184
  • MOL File:871543-07-6.mol
871543-07-6化学性质
  • 熔点 :182-184°C
  • 储存条件 :Hygroscopic, -20°C Freezer, Under Inert Atmosphere
  • 溶解度 :Methanol, Water
  • 形态 :Solid
  • 颜色 :White to Off-White
  • 稳定性 :Hygroscopic

871543-07-6性质、用途与生产工艺

  • 生物活性 H-1152 dihydrochloride 是一种膜通透的,选择性的 ROCK 抑制剂,Ki 值为 1.6 nM,对 ROCK2 的 IC50 值为 12 nM。
  • 靶点

    ROCKII

    12 nM (IC 50 )

    CaMKII

    0.18 μM (IC 50 )

    PKG

    0.36 μM (IC 50 )

    AuroraA

    0.745 μM (IC 50 )

    PKA

    3.03 μM (IC 50 )

    Src

    3.06 μM (IC 50 )

    PKC

    5.68 μM (IC 50 )

    Abl

    7.77 μM (IC 50 )

    MKK4

    16.9 μM (IC 50 )

    MLCK

    28.3 μM (IC 50 )

    EGFR

    50 μM (IC 50 )

    GSK3α

    60.7 μM (IC 50 )

    AMPK

    100 μM (IC 50 )

    P38α

    100 μM (IC 50 )

  • 体外研究

    H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC 50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC 50 s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively. H-1152 potently inhibits Rho kinase, with a K i of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with K i s of 0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 µM) highly inhibits MARCKS phosphorylation, with an IC 50 value of 2.5 µM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells. H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures.

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871543-07-6 试剂级价格
  • 更新日期:2024/11/08
  • 产品编号:HY-15720A
  • 产品名称:871543-07-6 H-1152 dihydrochloride
  • CAS编号:871543-07-6
  • 包装:2mg
  • 价格:950元
  • 更新日期:2024/11/08
  • 产品编号:HY-15720A
  • 产品名称:871543-07-6 H-1152 dihydrochloride
  • CAS编号:871543-07-6
  • 包装:5mg
  • 价格:1800元
871543-07-6生产厂家
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