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H-1152 dihydrochloride

Catalog No. T35328   CAS 871543-07-6
Synonyms: H-1152 2HCl, H-1152 dihydrochloride

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.

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H-1152 dihydrochloride Chemical Structure
H-1152 dihydrochloride, CAS 871543-07-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 58.00
2 mg In stock $ 84.00
5 mg In stock $ 145.00
10 mg In stock $ 273.00
25 mg In stock $ 527.00
50 mg In stock $ 765.00
100 mg In stock $ 1,070.00
500 mg In stock $ 2,150.00
1 mL * 10 mM (in DMSO) In stock $ 158.00
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Purity: 98.42%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 ROCK2 (cell-free assay):0.0120 μM, PKG (cell-free assay):0.360 μM, Aurora A (cell-free assay):0.745 μM, CaMK II (cell-free assay):0.180 μM, PKA (cell-free assay):3.03 μM
In vitro H-1152 dihydrochloride shows less inhibitory activities against Src, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC50s of 3.06, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively[1]. H-1152 dihydrochloride slightly suppresses PKA, PKC and MLCK, with Kis of 0.63, 9.27, and 10.1 μM, respectively. In LPA-treated cells, H-1152 dihydrochloride (0.1-10 µM) inhibits MARCKS phosphorylation (IC50 = 2.5 µM)[2]. H-1152 dihydrochloride (0.5-10 μM) does not decrease neuronal survival or alter the ratios of different neuronal morphologies. H-1152 dihydrochloride (10 μM) arguments neurite length in both BMP4 and LIF cultures[3].
Synonyms H-1152 2HCl, H-1152 dihydrochloride
Molecular Weight 392.34
Formula C16H23Cl2N3O2S
CAS No. 871543-07-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (114.7 mM ), Sonication is recommended.

H2O: 32.1 mg/mL (81.9 mM ), Sonication is recommended.

TargetMolReferences and Literature

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.  Content Brief 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.  Content Brief 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.  Content Brief

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library TGF-beta/Smad Compound Library Bioactive Compound Library Anti-Cancer Compound Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max

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Keywords

H-1152 dihydrochloride 871543-07-6 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK H-1152 2HCl H-1152 Dihydrochloride H 1152 H 1152 dihydrochloride H1152 Dihydrochloride H 1152 Dihydrochloride H1152 dihydrochloride H1152 H-1152 inhibitor inhibit

 

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