Ro 31-8220 (mesylate)

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Products Details

Product Description

– Ro 31-8220 mesylate 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.

Web ID

– HY-13866

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C26H27N5O5S2

Citations

– EMBO Mol Med. 2022 Dec 13;e16373.|Front Immunol. 2021 Feb 2;11:625542.|Harvard Medical School LINCS LIBRARY|Aging Cell. 2020 Oct;19(10):e13217.|Aging Cell. 2022 Feb 23;e13573.|Biomolecules. 2022, 12(3), 426.|FASEB J. 2019 Feb;33(2):2435-2450. |J Clin Invest. 2021 Dec 29;e150101.|Mol Med Rep. 2017 Nov;16(5):5924-5930.|Nat Commun. 2018 Sep 11;9(1):3688.|Neurogastroenterol Motil. 2020 Oct;32(10):1514-1528.

References

– [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.|[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.|[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.|[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.

CAS Number

– 138489-18-6

Molecular Weight

– 553.65

Compound Purity

– 99.28

SMILES

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

Clinical Information

– No Development Reported

Research Area

– Neurological Disease; Cardiovascular Disease; Cancer

Solubility

– DMSO : 35.71 mg/mL (ultrasonic)|H2O : 1 mg/mL (ultrasonic)

Target

– PKC

Isoform

– PKC;PKCα;PKCβ;PKCγ;PKCε

Pathway

– Epigenetics;TGF-beta/Smad

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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