Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

Catalog No.S7207 Synonyms: Bisindolylmaleimide IX Mesylate

For research use only.

Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 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.

Bisindolylmaleimide IX (Ro 31-8220 Mesylate) Chemical Structure

CAS No. 138489-18-6

Selleck's Bisindolylmaleimide IX (Ro 31-8220 Mesylate) has been cited by 21 publications

Purity & Quality Control

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Biological Activity

Description Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 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. [1] 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. [2] 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. [3] RO 31-8220 enhances epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. [4] 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. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 MUHGeY5kfGmxbjDhd5NigQ>? NETLc4lKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgbJVu[W5iTWPLNUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTBwMEC4{txO MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODl7OEO1NUc,OTB7OUizOVE9N2F-
Sf21 M330fWZ2dmO2aX;uJIF{e2G7 M4rwOWlvcGmkaYTpc44hd2ZiSHnzMZRi\2enZDDoeY1idiCJU1uzZkBmgHC{ZYPz[YQhcW5iU3[yNUBk\WyuczygTWM2OD1yLkCzPO69VQ>? NFXIRok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMEm5PFM2OSd-MUC5PVg{PTF:L3G+
HCT116 NE\rfJlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MmPEOFghcHK| NIP6XYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BwfmW{IHX4dJJme3OrbnegVnNMOiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvQDUQvF2= NYXYT3JWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0PFg3PjJpPkKxOFg5PjZ{PD;hQi=>
PC3 MnjVR5l1d3SxeHnjbZR6KGG|c3H5 NVPvNJh2PDhiaILz MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlc1|ryP MnfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2M{SxOFAoRjJ|NEO0NVQxRC:jPh?=
MDA-MB-231 M17rWmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXy0PEBpenN? MonHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KG:4ZYKg[ZhxemW|c3nu[{BTW0t{IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS55N988US=> M1\GcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEi4OlYzLz5{MUS4PFY3OjxxYU6=
MCF7 NFzWWYNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NHf0RmQ1QCCqcoO= Mm\TRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IH;2[ZIh\XiycnXzd4lv\yCUU1uyJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT65Ou69VQ>? NEPjb3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS4PFY3Oid-MkG0PFg3PjJ:L3G+
MCF7 M4fJVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NUnGVoNTPDhiaILz M33OV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjl4zszN NIH3Upo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{SzOFE1OCd-MkO0N|QyPDB:L3G+
DE3 M4jFXmZ2dmO2aX;uJIF{e2G7 NIfk[3JKdmirYnn0bY9vKG:oIHj1cYFvKG[3bHygcIVv\3SqIGPJVnQyKGW6cILld5Nm\CCrbjDESVMh[2WubIOgZpkh\my3b4LpcYV1emmlIHHzd4F6NCCLQ{WwQVI2|ryP Mn\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5M{SwOVAoRjF7N{O0NFUxRC:jPh?=
A549 MoTUSpVv[3Srb36gZZN{[Xl? NWDLRpFXUW6qaXLpeIlwdiCxZjDTTXJVOiCrbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGGkaXzpeJkhfG9iaX7keYNmKGi7cHXyZYNmfHmuYYTpc44hd2ZidIXieYxqdiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NVTlUlU1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexOFk5PjBpPkG3NVQ6QDZyPD;hQi=>
A549 NUTuZmd1TnWwY4Tpc44h[XO|YYm= M4nrNFExKHWP M3nocmlvcGmkaYTpc44hd2ZiU1nSWFIhcW5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bi[mmuaYT5JJRwKGmwZIXj[UBpgXCncnHj[ZR6dGG2aX;uJI9nKHS3YoXsbY4h[XRiMUCgeW0h[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NVrhS3VCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexOFk5PjBpPkG3NVQ6QDZyPD;hQi=>
MCF7 NWLhUY5YTnWwY4Tpc44h[XO|YYm= M4jkN|ExKHWP NWXtXHNnOTZiaILz MnPHTY5pcWKrdHnvckBw\iCVSWLUNkBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IIT1ZpVtcW5iaInw[ZJi[2W2eXzheIlwdiCjdDCxNEB2VSCjZoTldkAyPiCqcoOgZpkhX2W|dHXyckBjdG:2 M2LXcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEOwN|Q{Lz5{MECzNFM1OzxxYU6=
In vivo In MLP−/− Mice, Ro 31-8220 (6 mg/kg/d, s.c.) results in a significant increase in cardiac contractility. [6]

Protocol (from reference)

Kinase Assay:

[1]

  • Assay of PKC Activity :

    Assay mixtures contain 0.2 mg/mL peptide-gamma, 10 μM MgCl2, 0.6 mM CaCl2, 10 μM [γ-32P]ATP, 1.25 mg/mL phosphatidylserine and 1.25 ng/mL phorbol 12-myristate 13-acetate in 20 mM Hepes (pH 7.5), 2 mM EDTA, 1 mM dithiothreitol and 0.02% (w/v) Triton X-100. Peptide-γ is a synthetic peptide, GPRPLFCRKGSLRQKW, resembling the PKC-γ pseudosubstrate site, except that a serine residue replaces the pseudosubstrate alanine, converting the peptide from an inhibitor into a substrat. The assays are started by the addition of 2.5 m-units of enzyme, incubated at 30 °C for 10 min and terminated by spotting on to P81 paper, followed by extensive washing in 75 mM orthophosphoric acid. The papers are then washed in ethanol, dried, and incorporated radioactivity is determined by liquidscintillation spectroscopy.

Cell Research:

[3]

  • Cell lines: Human A549 lung and MCF-7 breast carcinoma cells
  • Concentrations: 2.5 μM
  • Incubation Time: 24-48 hours
  • Method:

    Human A549 lung and MCF-7 breast carcinoma cells are obtained from the European Collection of Animal Cell Cultures. Cells (passage number 10-30) are cultured in an atmosphere of 5% carbon dioxide, the former in Ham's F-12 medium with penicillin/streptomycin, the latter in minimum essential medium (Eagle's modification) with additional pyruvate (1 mM) and non-essential amino acids. Both media are supplemented with 10% FCS and glutamine (2 mM). Cells are subcultured routinely twice weekly to maintain logarithmic growth. For cell proliferation studies cells are seeded and incubated with 3 ml of medium including agents, which is replenished at intervals of 48 h (A549) or 72 h (MCF-7). Following incubation for 4 days (A549) or 6 days (MCF-7) with drugs, cell number is assessed using a Coulter Counter Model ZM. In order to achieve PKC depletion, cells are incubated for 24 h with bryostatin 1 (1 μM). Under these conditions growth inhibition caused by bryostatin 1 is negligible. Bryostatin is removed by extensive washing of the cells followed by a 2 h recovery period. In previous work using the A549 cell line this washing procedure has been shown to eliminate bryostatin-mediated effects. The cells are then incubated for a further 24 h with staurosporine, RO 31-8220, UCN-01 or H-7. In some experiments cells are incubated with inhibitor for 48 rather than 24 h, in this case bryostation was not removed and left in the incubate. After removal of agents inhibition of DNA synthesis is evaluated by measurement of [3H]Tdr incorporation into cell. Radioactivity is counted using a Packard 1500 Tricarb scintillation counter.

Animal Research:

[6]

  • Animal Models: MLP−/− Mice
  • Dosages: 6 mg/kg/d
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 553.65
Formula

C25H23N5O2S.CH4O3S

CAS No. 138489-18-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCSC(=N)N.CS(=O)(=O)O

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