General
Preferred name
H-1152 dihydrochloride
Synonyms
H-1152 2HCl ()
H 1152 dihydrochloride ()
H-1152 (dihydrochloride) ()
(S)-H-1152 (hydrochloride) ()
P&D ID
PD020291
CAS
871543-07-6
Tags
available
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 H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
PRICE 198
DESCRIPTION H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 ??M, 5.68 ??M, 0.360 ??M, 0.745 ??M and 0.180 ??M, respectively.
DESCRIPTION H-1152 Dihydrochloride is a cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases. It inhibits sulprostone-induced contractions in guinea pig aorta (IC50 = 190 nM) and displays proerectile effects in rats. It selectively blocks lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50=2.5nM) in NT-2 cells. (BOC Sciences Bioactive Compounds)
DESCRIPTION H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. (TargetMol Bioactive Compound Library)
DESCRIPTION Highly selective EGFR-kinase inhibitor (Tocris Bioactive Compound Library)
Compound Sets
7
Cayman Chemical Bioactives
EU-OPENSCREEN Bioactive Compound Library
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
External IDs
12
Properties
(calculated by RDKit )
Molecular Weight
391.09
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
2
Ring Count
3
Aromatic Ring Count
2
cLogP
2.76
TPSA
62.3
Fraction CSP3
0.44
Chiral centers
1.0
Largest ring
7.0
QED
0.85
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
ROCK2
ROCK
Aurora Kinase,CaMK,PKA,PKC,PKG,ROCK
Primary Target
Rho-Kinases
MOA
Inhibitor
Pathway
Cell Cycle/DNA Damage
cytoskeleton
Stem Cell/Wnt
TGF-beta/Smad
Cell Cycle/Checkpoint
Cytoskeletal Signaling
Stem Cells
Solubility
DMSO: ≥ 32 mg/mL
Source data