Ro 31-8220 (Synonyms: Bisindolylmaleimide IX)

製品番号: HY-13866A: Data Sheet 取扱説明書
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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. Ro 31-8220 can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Ro 31-8220 mesylate) that retains the same biological activity.

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CAS 番号 : 125314-64-9

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Other 在庫あり Forms of Ro 31-8220:

Ro 31-8220 mesylate Ro 31-8220 formic

Other Forms of Ro 31-8220:

Ro 31-8220 mesylate 在庫あり
Ro 31-8220 formic 在庫あり

顧客検証

: Ro 31-8220 purchased from MedChemExpress. 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 MedChemExpress. 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.

PKC アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

JNK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

JNK1 JNK2 JNK3 JNK

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製品説明

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)

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: 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]
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]
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]
Sf21	IC₅₀	38 nM Compound: Ro-318220	Inhibition of His-tagged human GSK3b expressed in Sf21 cells Inhibition of His-tagged human GSK3b expressed in Sf21 cells	[PMID: 10998351]
Sf9	IC₅₀	8 nM Compound: Ro-318220	Inhibition of His-tagged human MSK1 expressed in Sf9 cells Inhibition of His-tagged human MSK1 expressed in Sf9 cells	[PMID: 10998351]

体外実験

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].

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

体内実験

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].

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

分子量

457.55

分子式

C₂₅H₂₃N₅O₂S

CAS 番号

125314-64-9

SMILES

NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7. [Content Brief]

[2]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Content Brief]

[3]. Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20. [Content Brief]

[4]. Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82. [Content Brief]

[5]. Beltman J, et al. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996 Oct 25;271(43):27018-24. [Content Brief]

細胞実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7. [Content Brief] [2]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Content Brief] [3]. Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20. [Content Brief] [4]. Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82. [Content Brief] [5]. Beltman J, et al. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996 Oct 25;271(43):27018-24. [Content Brief]

Ro 31-8220 Related Classifications

Neurological Disease Cardiovascular Disease

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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 IXPKCJNKProtein kinase Cc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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Ro 31-8220 (Synonyms: Bisindolylmaleimide IX)

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Ro 31-8220 (Synonyms: Bisindolylmaleimide IX)

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Ro 31-8220 関連抗体

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PKC アイソフォーム固有の製品をすべて表示:

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生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Ro 31-8220 関連抗体

Ro 31-8220 Related Classifications

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