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Ro 31-8220 (formic)

CAT: 0804-HY-13866B-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13866B-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Ro 31-8220 formic 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 formic also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively) . Ro 31-8220 formic 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].
Product Name Alternative
Bisindolylmaleimide IX (formic)
UNSPSC
12352005
Target
JNK; PKC
Related Pathways
Epigenetics; MAPK/ERK Pathway; TGF-beta/Smad
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Purity
95.98
Solubility
DMSO : 100 mg/mL
Smiles
NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N.OC=O
Molecular Formula
C26H25N5O4S
Molecular Weight
503.57
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
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PKC; PKCα; PKCβ; PKCγ; PKCε

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