Bisindolylmaleimide V

Bisindolylmaleimide V Property

Melting point:

>260 °C

Boiling point:

655.7±55.0 °C(Predicted)

Density 

1.450±0.06 g/cm3(Predicted)

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

DMSO: soluble

form 

solid

pka

15.89±0.30(Predicted)

color 

Orange

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

CAS DataBase Reference

113963-68-1(CAS DataBase Reference)

Safety

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Bisindolylmaleimide V Chemical Properties,Usage,Production

Description

Ro 31-6045 (113963-68-1) is a bis indolylmaleimide derivative that is a potent inhibitor of the mitogen-stimulated protein kinase p70 (S6K) acting independently of its upstream activator mTOR.1?Does not inhibit PKC (at concentrations <100?mM) and therefore may be used as a negative control for bisindolylmaleimide PKC inhibitors2?such as GF 109203X3?and other structurally related inhibitors4.

Uses

Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 μM[1]. Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 of 8 μM[2].

Definition

ChEBI: Ro 31-6045 is a member of indoles.

References

[1] NELLY MARMY-CONUS  Richard B P  Katherine M Hannan. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70s6k/p85s6k: implications for the analysis of S6K signalling[J]. FEBS Letters, 2002, 519 1-3: 135-140. DOI:10.1016/s0014-5793(02)02738-2
[2] C S HARMON. Bisindolylmaleimide protein-kinase-C inhibitors delay the decline in DNA synthesis in mouse hair follicle organ cultures.[J]. Skin pharmacology : the official journal of the Skin Pharmacology Society, 1997, 10 2: 71-78. DOI:10.1159/000211471
[3] D. TOULLEC. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.[J]. The Journal of Biological Chemistry, 1991, 12 1: 15771-15781. DOI:10.1016/s0021-9258(18)98476-0
[4] PETER D. DAVIS. Inhibitors of protein kinase C. 1. 2,3-bisarylmaleimides[J]. Journal of Medicinal Chemistry, 1992, 35 1: 177-184. DOI:10.1021/jm00079a024