General
Preferred name
Bisindolylmaleimide VIII
Synonyms
RO 318161 ()
RO 31-7549 ()
Bis VIII ()
Ro 31-7549 acetate ()
Bis VIII acetate ()
Bisindolylmaleimide VIII (acetate) ()
Ro 31-7549 (acetate) ()
Bis VIII (acetate) ()
Bisindolylmaleimide VIII acetate ()
RO0317549-002 ()
P&D ID
PD008278
CAS
125313-65-7
138516-31-1
Tags
available
drug candidate
Drug Status
experimental
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 Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-¦Á, PKC-¦ÂI, PKC-¦ÂII, PKC-¦Ã, PKC-¦Å, respectively[1]. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2].
PRICE 139
DESCRIPTION Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-??, PKC-??I, PKC-??II, PKC-??, and PKC-??, respectively.
PRICE 879
DESCRIPTION Bisindolylmaleimide VIII (Ro-31-7549) is a selective and potent protein kinase C (PKC) inhibitor with good inhibition of PKC-??, PKC-?? I, PKC-?? II, PKC-??, and PKC-??.Bisindolylmaleimide VIII Bisindolylmaleimide VIII inhibits T cell-mediated autoimmune diseases and enhances Fas-mediated apoptosis through a protein kinase C-independent mechanism.
DESCRIPTION Bisindolylmaleimide VIII (BIM VIII) is a selective protein kinase C (PKC) inhibitor with IC50 of 158 nM for rat brain that acts at the ATP binding site. Bis VIII has been previously shown to enhance Fas-mediated apoptosis through a protein kinase C-independent mechanism. BIM VIII does not inhibit the tyrosine phosphorylation or the activation of phospholipase C γ1. BIM VIII inhibits carbachol-evoked noradrenaline release from human SH-SY5Y neuroblastoma cells with an IC50 of 600 nM. (BOC Sciences Bioactive Compounds)
DESCRIPTION Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively. (TargetMol Bioactive Compound Library)
DESCRIPTION Bisindolylmaleimide VIII (Ro-31-7549) is a selective and potent protein kinase C (PKC) inhibitor with good inhibition of PKC-α, PKC-β I, PKC-β II, PKC-γ, and PKC-ε.Bisindolylmaleimide VIII Bisindolylmaleimide VIII inhibits T cell-mediated autoimmune diseases and enhances Fas-mediated apoptosis through a protein kinase C-independent mechanism. (TargetMol Bioactive Compound Library)
Compound Sets
9
BOC Sciences Bioactive Compounds
bisindolylmaleimide-viii-acetate-salt-cas-138516-31-1-item-122286
Cayman Chemical Bioactives
13333
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
CZ-OPENSCREEN Bioactive Library
DrugBank
DB01946
MedChem Express Bioactive Compound Library
HY-129624A
Novartis Chemogenetic Library (NIBR MoA Box)
TargetMol Bioactive Compound Library
T10549
T71125
ZINC Tool Compounds
ZINC000002011710
External IDs
35
Properties
(calculated by RDKit )
Molecular Weight
398.17
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
3.05
TPSA
82.05
Fraction CSP3
0.17
Chiral centers
0.0
Largest ring
6.0
QED
0.51
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Apoptosis
PKC
PKCα
PKCβ1
PKCβ2
PKCγ
PKCε
PRKC
Member status
member
MOA
Non-Steroidal Antiinflammatory Drugs
Protein Kinase C (PKC) Inhibitors
Pathway
Chromatin/Epigenetic
Cytoskeletal Signaling
Epigenetics
TGF-beta/Smad
Solubility
Soluble in DMSO, methanol, water, and ethanol (slightly).
Source data