1H-Pyrrole-2,5-dione, 3-[8-(aMinoMethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-Methyl-1H-indol-3-yl)-, Monohy Chemical Properties

storage temp. 

under inert gas (nitrogen or Argon) at 2-8°C

solubility 

Soluble in DMSO (up to 10 mg/ml)

form 

Red solid.

color 

Red

biological source

synthetic (organic)

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

1H-Pyrrole-2,5-dione, 3-[8-(aMinoMethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-Methyl-1H-indol-3-yl)-, Monohy Usage And Synthesis

Description

Ro 31-8425 (145317-11-9) is a selective, reversible, ATP-competitive inhibitor of protein kinase C. Inhibits PKCα, β1, β2, γ and ε, IC50= 8, 8, 14,13 and 39 nM respectively.1? Extremely useful tool for probing PKC-dependent physiology2 or signaling pathways3. Increases MSC adhesion to an ICAM-1 coated substrate in vitro and enables targeted delivery of systematically administered MSCs to inflamed sites in vivo in a CD11a-dependent manner.4? Cell permeable.

Uses

Bisindolylmaleimide X hydrochloride is a potent and selective cell-permeable protein kinase C (PKC) inhibitor. Studies reveal that inhibition of PKCα by Bisindolylmaleimide X and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure.

IC 50

PKC; CDK2: 200 nM (IC₅₀)

References

[1] S E WILKINSON  J S N  P J Parker. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.[J]. Biochemical Journal, 1993, 294 ( Pt 2): 335-337. DOI:10.1042/bj2940335
[2] WENYAN NIU. PKCε regulates contraction-stimulated GLUT4 traffic in skeletal muscle cells†[J]. Journal of Cellular Physiology, 2010, 226 1: 173-180. DOI:10.1002/jcp.22320
[3] JOSE M JIMENEZ-LOPEZ A I C. Protein kinase C signaling as a survival pathway against CYP2E1-derived oxidative stress and toxicity in HepG2 cells.[J]. Journal of Pharmacology and Experimental Therapeutics, 2005, 312 3: 998-1006. DOI:10.1124/jpet.104.076737
[4] OREN LEVY. A small-molecule screen for enhanced homing of systemically infused cells.[J]. Cell reports, 2015, 10 8: 1261-1268. DOI:10.1016/j.celrep.2015.01.057

1H-Pyrrole-2,5-dione, 3-[8-(aMinoMethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-Methyl-1H-indol-3-yl)-, Monohy(145317-11-9)Related Product Information

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