General
Preferred name
(-)-Indolactam V
Synonyms
INDOLACTUM ()
Indolactam V ()
P&D ID
PD018958
CAS
90365-57-4
132341-58-3
Tags
available
drug candidate
Drug indication
Discovery agent
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 ¦ÌM for ¦Ç-CRD2 (PKC¦Ç surrogate peptide), ¦Ã-CRD2 (PKC¦Ã surrogate peptide), and Kds of 5.5 nM (¦Ç-C1B), 7.7 nM (¦Å-C1B), 8.3 nM (¦Ä-C1B), 18.9 nM (¦Â-C1A-long), 20.8 nM (¦Á-C1A-long), 137 nM (¦Â-C1B), 138 nM (¦Ã-C1A), 213 nM (¦Ã-C1B), and has antitumor activity.
DESCRIPTION
(-)-Indolactam V is an indole alkaloid compound which activates protein kinase C (PKC), which strongly directs human ES cell-derived definitive endoderm into pancreatic endoderm. It is weak tumor promoter. It binds to PKC regulatory domains of mouse skin PKCη and rat brain PKCγ with Ki values of 3.4 nM and 1 μM, respectively. It induces differentiation of human embryonic stem cells into pancreatic progenitors through activation of PKC signaling at 1 μM. It may be used as an effective diabetes therapy. It may share an RA-dependent signaling pathway, allowing ultimately to streamline the process of efficient pancreatic endoderm derivation. It was predicted to be a biosynthetic intermediate and was confirmed via in vitro prenylation by LtxC due to the structural relatedness of the lyngbyatoxins and teleocidin. It induces differentiation of a substantial number of Pdx1-expressing cells from human ESCs.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
1
Compound Sets
6
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
DrugMAP
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
24
Molecular Weight
301.18
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
3
Rotatable Bonds
2
Ring Count
3
Aromatic Ring Count
2
cLogP
1.66
TPSA
68.36
Fraction CSP3
0.47
Chiral centers
2.0
Largest ring
9.0
QED
0.79
QED
0.79
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Member status
member
MOA
PKC agonist
Target
PKC
Pathway
Epigenetics
TGF-beta/Smad
Solubility
10 mM in DMSO
Source data

