General
Preferred name
Ro31-8220
Synonyms
Ro 31-8220 Mesylate ()
BISINDOLYLMALEIMIDE IX ()
RO 31-8220 ()
Ro 31-8220 methanesulfonate ()
Bisindolylmaleimide IX Mesylate ()
Bisindolylmaleimide IX (mesylate) ()
PMID28460551-Compound-3 ()
Ro 31-8220 (mesylate) ()
Ro 31-8220 (formic) ()
Bisindolylmaleimide IX (formic) ()
RO0318220-000 ()
RO-318220 mesylate ()
Bisindolylmaleimide IX (Ro 31-8220 Mesylate) ()
P&D ID
PD038906
CAS
138489-18-6
125314-64-9
Tags
available
drug candidate
nuisance
Drug indication
Discovery agent
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKC¦Á, PKC¦ÂI, PKC¦ÂII, PKC¦Ã, PKC¦Å and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3¦Â (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
PRICE 168
DESCRIPTION Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-??/??I/??II/??/?? (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3??.
DESCRIPTION SERCA ATPase blocker. Also potent BKCa channel blocker (Tocris Bioactive Compound Library)
DESCRIPTION Protein kinase inhibitor (Tocriscreen Plus)
DESCRIPTION Protein kinase inhibitor (Tocriscreen Total)
DESCRIPTION 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. (BOC Sciences Bioactive Compounds)
DESCRIPTION Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β. (TargetMol Bioactive Compound Library)
DESCRIPTION Ro 31-8220 is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate or diacylglycerols by 95%. Ro-31-8220 showed the apoptotic effect on HL-60 cells, which was mediated by a well-characterized transduction process of apoptotic signals. Moreover, the ability of Ro-31-8220 to induce apoptotic activation was completely inhibited by the over-expression of the apoptotic suppressor gene, Bcl-2, in the cells. (BOC Sciences Bioactive Compounds)
Cell lines
4
Organisms
0
Compound Sets
17
AdooQ Bioactive Compound Library
A13514
BOC Sciences Bioactive Compounds
ro-31-8220-mesylate-cas-138489-18-6-item-84-209255
ro31-8220-cas-125314-64-9-item-84-196598
Cayman Chemical Bioactives
13334
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DMA1FRM
DMDJLF0
EU-OPENSCREEN Bioactive Compound Library
EOS101001
Guide to Pharmacology
5259
LINCS compound set
10407-103
MedChem Express Bioactive Compound Library
HY-13866
HY-13866B
Nuisance compounds in cellular assays
Selleckchem Bioactive Compound Library
ro-31-8220-mesylate
TargetMol Bioactive Compound Library
T6643
Tocris Bioactive Compound Library
2002
Tocriscreen Plus
2002
Tocriscreen Total
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
457.16
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
6
Ring Count
5
Aromatic Ring Count
4
cLogP
3.72
TPSA
105.9
Fraction CSP3
0.16
Chiral centers
0.0
Largest ring
6.0
QED
0.18
Structural alerts
3
aggregator (Aggregator Advisor)
Aggregators
aggregator (ZINC)
Aggregators
Optical interference
Fluorescence
Nuisance compounds
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
PKC
PKCα
PKCβ1
PKCβ2
PKCγ
PKCε
AKT1, GSK3B, LCK, MAPK1, MAPK11, MAPK12, MAPK14, MAPK8, PRKCA, ROCK1, RPS6KB1, SIRT1
JNK
PRKC
Pathway
TGF-beta/Smad
Epigenetics
Chromatin/Epigenetic
Cytoskeletal Signaling
MAPK/ERK Pathway
Primary Target
Broad Spectrum Protein Kinase Inhibitors
MOA
Inhibitor
PKC inhibitor
Source data