General
Preferred name
FASUDIL
Synonyms
FASUDIL HYDROCHLORIDE ()
Hexahydro-1-(5-isoquinolylsulfonyl)-1h-1,4-diazepine ()
HA-1077, AT-877, ZK-258594 ()
Fasudil (HA-1077) HCl ()
AT-877 hydrochloride ()
Fasudil HCl ()
HA-1077 hydrochloride ()
HA-1077 ()
AT877 ()
Fasudil HCl (HA-1077) ()
fasudil ER ()
Fasudil (Hydrochloride) ()
Fasudil (dihydrochloride) ()
HA-1077 (hydrochloride) ()
AT-877 (Hydrochloride) ()
HA-1077 (dihydrochloride) ()
AT-877 (dihydrochloride) ()
AT-877,HA-1077 HCl ()
HA-1077 dihydrochloride ()
Fasudil (ha-1077) hydrochloride ()
AT 877 ()
AT-877 ()
HA 1077 ()
NSC-759827 ()
ZK-258594 ()
Fasudil ()
Eril ()
P&D ID
PD001304
CAS
103745-39-7
105628-07-7
203911-27-7
Tags
available
drug
drug candidate
Approved by
PMDA
First approval
1995
Drug indication
Discovery agent
Cardiovascular disease
Drug Status
approved
investigational
Max Phase
2.0
3.0
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 Fasudil is a potent inhibitor of the Rho-kinases ROCK1 and ROCK2. (GtoPdb)
PRICE 29
DESCRIPTION Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 ¦ÌM for ROCK1, IC50s of 0.158 ¦ÌM and 4.58 ¦ÌM, 12.30 ¦ÌM, 1.650 ¦ÌM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].
PRICE 29
DESCRIPTION Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 ??M, 1.0 ??M, 9.3 ??M and 55 ??M, respectively.
DESCRIPTION Fasudil is a potent inhibitor of the Rho-kinases ROCK1 and ROCK2. (PKIDB)
DESCRIPTION Fasudil is a potent and selective Rho-kinase (ROCK) inhibitor and vasodilator. ROCK is an enzyme that participates in vasoconstriction and vascular remodeling. Fasudil is used for the treatment of cerebral vasospasm and has the potential to treat pulmonary hypertension as well as certain memory loss. (BOC Sciences Bioactive Compounds)
DESCRIPTION Fasudil is a nonspecific ROCK inhibitor and also has an inhibitory effect on protein kinases. Fasudil is also a potent Ca2+channel antagonist and vasodilator. (Enamine Bioactive Compounds)
DESCRIPTION Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK. (TargetMol Bioactive Compound Library)
DESCRIPTION HA-1077 is a potent and selective inhibitor of Rho kinase (ROCK). HA-1077 exhibited neuroprotective effects and enhanced cognition in mouse models of amyotrophic lateral sclerosis (ALS), suggesting its potential use for cognitive disorders such as ALS, Alzheimer's disease and spinal muscular atrophy. It also suppresses tumor cell motility and metastasis. (BOC Sciences Bioactive Compounds)
DESCRIPTION Protein kinase inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Inhibitor of cyclic nucleotide dependent- and Rho-kinases (Tocriscreen Plus)
DESCRIPTION Inhibitor of cyclic nucleotide dependent- and Rho-kinases (Tocriscreen Total)
DESCRIPTION Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
1
Compound Sets
34
AdooQ Bioactive Compound Library
A10381
BOC Sciences Bioactive Compounds
fasudil-cas-103745-39-7-item-53397
fasudil-dihydrochloride-cas-203911-27-7-item-181028
Cayman Chemical Bioactives
10010559
ChEMBL Drugs
CHEMBL38380
CHEMBL541388
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5181
Concise Guide to Pharmacology 2019/20
5181
Concise Guide to Pharmacology 2021/22
5181
Concise Guide to Pharmacology 2023/24
5181
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08162
DrugCentral
1132
DrugCentral Approved Drugs
1132
DrugMAP
DMTCNOM
DrugMatrix
Enamine Bioactive Compounds
EBC-00589
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101813
Guide to Pharmacology
5181
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL38380
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL38380
MedChem Express Bioactive Compound Library
HY-10341C
HY-10341
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Other bioactive compounds
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Fasudil-HCl(HA-1077)
TargetMol Bioactive Compound Library
T1606
T3060
The Spectrum Collection
Tocris Bioactive Compound Library
0541
Tocriscreen Plus
0541
Tocriscreen Total
External IDs
70
Properties
(calculated by RDKit )
Molecular Weight
291.1
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
2
Ring Count
3
Aromatic Ring Count
2
cLogP
1.22
TPSA
62.3
Fraction CSP3
0.36
Chiral centers
0.0
Largest ring
7.0
QED
0.9
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Pathway
TGF-beta/Smad
Stem Cell/Wnt
Cell Cycle/DNA Damage
Neuronal Signaling
Autophagy
Cell Cycle/Checkpoint
Chromatin/Epigenetic
Cytoskeletal Signaling
Membrane Transporter/Ion Channel
Metabolism
Microbiology/virology
Proteases/Proteasome
Stem Cells
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Epigenetics
Anti-infection
cytoskeleton
Targets
ROCK2,PRKACA,PRKACB,PRKACG,PRKCA,PRKCB,PRKCZ,PRKCH,PRKCG,PRKCD,PRKCI,PRKCE,PRKG1,PRKG2,MYLK
Primary Target
Rho-Kinases
MOA
PKA inhibitor
PKC inhibitor
ROCK inhibitor
Serine/threonin kinase inhibitor
Inhibitor
Calcium Sensitizers
Rho Kinase Inhibitors
rho associated kinase inhibitor
Member status
member
Target
PKIA, PRKACA, ROCK1, ROCK2
Autophagy,Calcium Channel,MLCK,PKA,PKC,PKG,Rho,ROCK
Calcium Channel
HIV
PKA
PKC
ROCK
MLCK
PKG
ROCK2
Indication
cerebral vasospasm
Solubility
In vitro:<br/>10 mM in DMSO
Source data