[CAS NO. 871543-07-6] H-1152dihydrochloride
PRODUCTS SPECIFICATIONS [871543-07-6]
DESCRIPTION [871543-07-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 392.34 |
| Molecular Formula | C16H23Cl2N3O2S |
| SMILES | CC1=CN=CC2=C1C(S(=O)(N3[C@@H](C)CNCCC3)=O)=CC=C2.[H]Cl.[H]Cl |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
ROCKII 12 nM (IC 50 ) |
CaMKII 0.18 μM (IC 50 ) |
PKG 0.36 μM (IC 50 ) |
AuroraA 0.745 μM (IC 50 ) |
PKA 3.03 μM (IC 50 ) |
Src 3.06 μM (IC 50 ) |
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|
PKC 5.68 μM (IC 50 ) |
Abl 7.77 μM (IC 50 ) |
MKK4 16.9 μM (IC 50 ) |
MLCK 28.3 μM (IC 50 ) |
EGFR 50 μM (IC 50 ) |
GSK3α 60.7 μM (IC 50 ) |
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AMPK 100 μM (IC 50 ) |
P38α 100 μM (IC 50 ) |
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In Vitro
H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC 50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC 50 s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively [1] . H-1152 potently inhibits Rho kinase, with a K i of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with K i s of 0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 µM) highly inhibits MARCKS phosphorylation, with an IC 50 value of 2.5 µM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells [2] . H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 127.44 mM ; Need ultrasonic)
H 2 O : 35.71 mg/mL ( 91.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5488 mL | 12.7440 mL | 25.4881 mL |
| 5 mM | 0.5098 mL | 2.5488 mL | 5.0976 mL |
| 10 mM | 0.2549 mL | 1.2744 mL | 2.5488 mL |
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1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (127.44 mM); Clear solution; Need ultrasonic
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2.
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3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
References
- [1] Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52. Epub 2005 Sep 12.
- [2] Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16.
- [3] Lie M, et al. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010 Aug 25;169(2):855-62.