Ro 31-8220

CAT: 0804-HY-13866ASize: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-13866ASize:1 Each
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Description
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[1][2][3][4][5].
CAS Number
[125314-64-9]
Product Name Alternative
Bisindolylmaleimide IX
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
Target
JNK; PKC
Type
Reference compound
Related Pathways
Epigenetics; MAPK/ERK Pathway; TGF-beta/Smad
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/ro-31-8220.html
Solubility
10 mM in DMSO
Smiles
NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N
Molecular Formula
C25H23N5O2S
Molecular Weight
457.55
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501
References & Citations
[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.|[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PKC; PKCα; PKCβ; PKCγ; PKCε
Citation 01
Aging Cell. 2020 Oct;19 (10) :e13217.|Aging Cell. 2022 Mar;21 (3) :e13573.|Biomolecules. 2022 Mar 10;12 (3) :426.|FASEB J. 2019 Feb;33 (2) :2435-2450. |J Clin Invest. 2022 Feb 15;132 (4) :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.|bioRxiv. 2024 Jul 25.|EMBO Mol Med. 2023 Jan 11;15 (1) :e16373.|Front Immunol. 2021 Feb 2:11:625542.|Harvard Medical School LINCS LIBRARY|Life Metab. 2025 Jan 29;4 (2) :loaf002.

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