General
Preferred name
Icerguastat
Synonyms
Sephin 1 ()
lcerguastat ()
IFB-088 ()
(E/Z)-Icerguastat ()
Sephin1 ()
(E/Z)-Sephin1 ()
(E/Z)-IFB-088 ()
NSC-65390 ()
Sephin-1 ()
IFB-088 acetate ()
P&D ID
PD016352
CAS
1883549-35-6
13098-73-2
951441-04-6
469866-31-7
Tags
available
drug candidate
Drug Status
investigational
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Icerguastat (IFB-088, Sephin1) selectively inhibits the regulatory subunit PPP1R15A within the PPP1R15A/PP1c phosphatase complex . Inhibiting PPP1R15A results in reduced dephosphorylation of the translation initiation factor eIF2α, which rescues cells from proteostasis collapse. Structurally icerguastat is a derivative but it has no α2-adrenerceptor agonist activity. Icerguastat is designed to maintain an active integrated stress response as a cytoprotective mechanism to combat the toxic effects of cellular stress .
(GtoPdb)
DESCRIPTION
Icerguastat (Sephin1), a derivative of Guanabenz lacking the ¦Á2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2¦Á dephosphorylation, thereby prolonging the protective response. Anti-prion effect[1][2][3].
DESCRIPTION
(E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research[1].
PRICE
29
PRICE
110
DESCRIPTION
IFB-088 acetate, a benzyl guanidine derivative, is used to treat diseases and cancers associated with the PPP1R15A pathway and associated with protein misfolding stress, Examples include tau disease, synaptic riboprotein disease, polyglutamine and polyalanine diseases, leukodystrophy, cystic fibrosis, multiple sclerosis, lysosome storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardiovascular diseases, osteoporosis, neurological trauma, and more.
DESCRIPTION
Sephin 1 is a selective PPP1R15A inhibitor devoid of PPP1R15B and α2-adrenergic activity. In cells, Sephin 1 selectively disrupted the PPP1R15A-PP1c complex, thus prolonging eIF2α phosphorylation after stress, delaying translation recovery, and attenuated expression of stress genes such as the pro-apoptotic protein CHOP. In mice, Sephin 1 safely prevented the motor, morphological, and molecular defects of two otherwise unrelated protein-misfolding diseases.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Icerguastat (IFB-088) is a selective inhibitor of holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Highly potent and selective renin inhibitor
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
13
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
DrugBank
Guide to Pharmacology
Mcule NIBR MoA Box Subset
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
27
Molecular Weight
196.05
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
3
Rotatable Bonds
2
Ring Count
1
Aromatic Ring Count
1
cLogP
1.16
TPSA
74.26
Fraction CSP3
0.0
Chiral centers
0.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
phosphatase
phosphatase PPP1R15A
PPP1R15A inhibitor
Primary Target
Protein Ser/Thr Phosphatases
MOA
Inhibitor
sustains UPR
Member status
member
Pathway
Metabolic Enzyme/Protease
Metabolism
Source data
