[CAS NO. 138489-18-6] Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

Name: Bisindolylmaleimide IX (Ro 31-8220 Mesylate)
Brand: Arctom Scientific
SKU: SLK-S7207

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PRODUCTS SPECIFICATIONS [138489-18-6]

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Catalog

SLK-S7207

Brand

Selleck

CAS

138489-18-6

DESCRIPTION [138489-18-6]

Overview

MDL	MFCD03788207
Molecular Weight	553.65
Molecular Formula	C25H23N5O2S.CH4O3S
SMILES	S(C)(=O)(=O)O.O=C1C(C=2C=3C(N(CCCSC(=N)N)C2)=CC=CC3)=C(C(=O)N1)C=4C=5C(N(C)C4)=CC=CC5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8062 mL	9.0310 mL	18.0620 mL
5 mM	0.3612 mL	1.8062 mL	3.6124 mL
10 mM	0.1806 mL	0.9031 mL	1.8062 mL
50 mM	0.0361 mL	0.1806 mL	0.3612 mL

Description

Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan- inhibitor with of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.

Targets

PKCα ^[1] (Cell-free assay)	PKCβ2 ^[1] (Cell-free assay)	PKCβ1 ^[1] (Cell-free assay)	PKCε ^[1] (Cell-free assay)	PKCγ ^[1] (Cell-free assay)
5 nM	14 nM	24 nM	24 nM	27 nM

In vitro

Ro 31-8220 inhibits rat brain PKC activity with IC50 of 23 nM, and does not show any high degree of selectivity between PKC-α, PKC-β, PKC-γ, and PKC-ε. Ro 31-8220 also inhibits MSK1, MAPKAPK1, RSK, GSK3β and S6K1 with a potency similar to that for PKC. In addition, Ro 31-8220 inhibits voltage-dependent Na+ channels. Ro 31-8220 alters cellular protein kinase C localization and potently inhibits growth of A549 and MCF-7 cells with IC50 of 0.78 μM and 0.897 μM, respectively. RO 31-8220 enhances epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. Ro 31-8220 significantly decreases apoE secretion from primary human macrophages by inhibiting vesicular transport of apoE to the plasma membrane without significantly affecting apoE mRNA or apoE protein levels.

In vivo

In MLP−/− Mice, Ro 31-8220 (6 mg/kg/d, s.c.) results in a significant increase in cardiac contractility.

References

[1] Wilkinson SE, et al. Biochem J. 1993, 294 ( Pt 2), 335-337.
[2] Davies SP, et al. Biochem J. 2000, 351(Pt 1), 95-105.
[3] Courage C, et al. Br J Cancer. 1995, 71(4), 697-704.
[4] Kim SY, et al. BMB Rep. 2011, 44(2), 140-145.
[5] Karunakaran D, et al. J Biol Chem. 2013, 288(7), 5186-5197.
[6] Hambleton M, et al. Circulation. 2006, 114(6), 574-582.

Synonyms

Carbamimidothioic acid, 3-[3-[2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl ester, methanesulfonate (1:1)

Carbamimidothioic acid, 3-[3-[2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl ester, monomethanesulfonate

Ro 31-8220 methanesulfonate

Ro 31-8220 mesylate

Methanesulfonic acid 3-[3-[4-(1-methylindol-3-yl)-2,5-dioxopyrrol-3-yl]indol-1-yl]propyl carbamimidothioate