2. Epigenetics TGF-beta/Smad
  3. PKC
  4. Ro 31-8220

Ro 31-8220  (Synonyms: Bisindolylmaleimide IX)

目录号: HY-13866A
产品使用指南

摩尔计算器

Ro 31-8220 是一种有效的 PKC 抑制剂，对 PKCα，PKCβI，PKCβII，PKCγ，PKCε 和大鼠大脑 PKC 的 IC50 值为 5，24，14，27，24 和 23 nM，同时能够有效抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β (IC50，3，8，15，38 nM), 对 MKK3，MKK4，MKK6 和 MKK7 无作用。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 Ro 31-8220 mesylate。

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Ro 31-8220 Chemical Structure

Ro 31-8220 Chemical Structure

CAS No. : 125314-64-9

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Ro 31-8220 的其他形式现货产品:

Other Forms of Ro 31-8220:

Ro 31-8220 相关抗体

Top Publications Citing Use of Products

    Ro 31-8220 purchased from MCE. Usage Cited in: Nat Commun. 2018 Sep 11;9(1):3688.  [Abstract]

    Levels of phosphorylated FAK and AKT are reduced by the PKN1 inhibitors. Cells are seeded in six-well plates after transfection with PKN1 inhibitors Lestaurtinib and Ro318220 or DMSO as control.

    Ro 31-8220 purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Nov;16(5):5924-5930.  [Abstract]

    The PKC inhibitor Ro 31 8220 is used to investigate the implication of PKC mediated signaling pathways.

    查看 PKC 亚型特异性产品:

    查看所有亚型
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

    IC50 & Target[1][2]

    PKC-α

    5 nM (IC50)

    PKC-βII

    14 nM (IC50)

    PKC-βI

    24 nM (IC50)

    PKC-ε

    24 nM (IC50)

    PKC-γ

    27 nM (IC50)

    Rat Brain PKC

    23 nM (IC50)

    MAPKAP-K1b

    3 nM (IC50)

    MSK1

    8 nM (IC50)

    S6K1

    15 nM (IC50)

    GSK3β

    38 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 IC50
    0.84 μM
    Compound: 4, Ro-318220
    Antiproliferative activity against human HCT116 cells over expressing RSK2 after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells over expressing RSK2 after 48 hrs by MTT assay
    		[PMID: 21488662]
    MCF7 IC50
    1.96 μM
    Compound: Ro31-8220
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay
    		[PMID: 23434140]
    MCF7 IC50
    1.96 μM
    Compound: 4, Ro-318220
    Antiproliferative activity against human MCF7 cells over expressing RSK2 after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells over expressing RSK2 after 48 hrs by MTT assay
    		[PMID: 21488662]
    MDA-MB-231 IC50
    1.77 μM
    Compound: 4, Ro-318220
    Antiproliferative activity against human MDA-MB-231 cells over expressing RSK2 after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells over expressing RSK2 after 48 hrs by MTT assay
    		[PMID: 21488662]
    PC-3 IC50
    1.74 μM
    Compound: Ro31-8220
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
    		[PMID: 23434140]
    体外研究
    (In Vitro)

    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively[1]. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na+ channels[2]. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Ro 31-8220 相关抗体:
    体内研究
    (In Vivo)

    Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP−/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    457.55

    Formula

    C25H23N5O2S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献
    Cell Assay
    [1]

    A neurotoxic concentration of paraoxon (200 μM) is added to the granule cell cultures for the indicated time on day in vitro (DIV) 8. The following drugs are added to the granule cell cultures prior to or after paraoxon exposure on DIV 8: Ro-81-3220 (1 μM) is added 15 min prior to or 3 h after the addition of paraoxon. TPA (0.1 μM) is added 15 min prior to the addition of paraoxon[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice[4]
    The affects of long-term Ro 31-8220 administration over 4 to 6 weeks in MLP−/− heart failure mice are investigated. All mice are assessed for ventricular performance by echocardiography at the beginning of the study and 6 weeks later. Ro 31-8220 (or vehicle) is injected subcutaneously once per day at a dosage of 6 mg/kg/d[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Ro 31-8220 相关分类

    • 摩尔计算器

    • 稀释计算器

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ro 31-8220125314-64-9Bisindolylmaleimide IXPKCProtein kinase CInhibitorinhibitorinhibit

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