home · products · checkout · contact  
 
  PRODUCT DETAILS      
Shopping cart  Shopping cart
0 Product(s) in cart
Total $0.00
> Checkout
Login Status  Login Status

Not logged in

» Login

Copyright © 2008
SuperNova Life Science

 

Home » PhotoChems™ (Search By Pathway) » Second Messenger Effectors » PKC

 Checkout
Ro-31-8220  
Ro-31-8220

Caged at red
Size: 100 μl
Concentration: 1 mM

Heat Map / Heat Map Guide

A multi-kinase inhibitor used generally as a PKC inhibitor in the literature, and less commonly as an inhibitor of p70S6K and GSK-3. In an extended cell-free assay of 110 kinases, the top 10 inhibited kinases in decreasing order of predicted potency were (IC50, nM): GSK-3β (2), PKCα (6), SLK (10), RSK isoforms (15-23), PKN2 (16), PIM1 (18), CLK1 (19), MSK1 (23), p70S6K (40) and CDK2 (44). In cells, it is a cell-permeable and competitive inhibitor of PKC (IC50 = 10 nM) over CaMKII (IC50 = 17 μM) and PKA (IC50 = 900 nM). It inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and GSK-3β in immunoprecipitates (IC50 = 2.8 nM). It inhibits EGF-induced activation of p70S6K in mouse fibroblasts (IC50 = 600 nM), but not in adult rat ventricular myocytes up to 1 μM. Other known PKC-independent effects include: (1) preventing growth factor induced expression of MAP kinase phosphatase-1 (MKP1/CL100) and the transcription factor c-Fos in rat fibroblasts, (2) JNK1 activation even after PKC down-regulation, possibly a secondary result of reduced MKP1 (a negative regulator of JNK), and (3) inhibition of the phosphorylation of Raf-1 and induction of apoptosis, independent of its effects on PKC, in HL-60 cells.

References

Roberts NA, Marber MS, Avkiran M. (2004) Specificity of action of bisindolylmaleimide PKC inhibitors: do they inhibit the 70kDa ribosomal S6 kinase (p70S6K) in cardiac myocytes? Biochem Pharmacol. 68(10):1923-8; Marmy-Conus N, Hannan KM, Pearson RB. (2002) Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70(s6k)/p85(s6k): implications for the analysis of S6K signalling. FEBS Lett. 519(1-3):135-40; Powell, D.J., et al. 2003. Mol. cell Biol. 23, 7794. Han, Z., et al. 2000. Cell Death Differ. 7, 521. Hers, I., et al. 1999. FEBS Lett. 460, 433. Alessi, D.R., 1997. The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase-1beta (Rsk-2) and p70 S6 kinase. FEBS Lett. 402(2-3):121; Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018. Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun. 194, 1111. McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol. 46, 583. Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.

Price: $44.50

Caged: YesNo

« Previous | Next »


Email Friend


Product Spotlights

· Light Activation Instruments

· PhotoMorphs™

· PhotoChems™

· Custom Caging

Technical Resources

· Over 2000 annotated PhotoMorph™sequences

· IC50 Heat Maps

· Navigate products by signaling pathway

· Target Ortholog Maps

logo
SuperNova
Life Science

215 Clay Street
Suite B6
Auburn, WA
98001 USA
877-300-NOVA

E-mail:
Orders
Support

Hours:
8 am - 5 pm PST

 
home | products | checkout | contact