H-1152 dihydrochloride CAS: 451462-58-1
MF: C16H21N3O2S•2HCl
MW: 392.34
A cell permeable, highly specific, and potent ATP-competitive inhibitor of ρ-kinase inhibitor.

H-1152 dihydrochloride (CAS 451462-58-1)

H-1152 dihydrochloride | CAS 451462-58-1 is rated 5.0 out of 5 by 1.
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Alternate Names: (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine . 2HCl
Application: H-1152 dihydrochloride is a cell permeable, highly specific, and potent ATP-competitive inhibitor of ρ-kinase inhibitor
CAS Number: 451462-58-1
Purity: ≥98%
Molecular Weight: 392.34
Molecular Formula: C16H21N3O2S•2HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

H-1152 . dihydrochloride is a selective ATP-competitive inhibitor of rho-kinase (ROCK) inhibitor, cell permeable, highly specific, and potent (Ki = 1.6 nM). Exhibits weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27mM for PKC and 10.1 mM for MLCK) and is more potent and selective than Y-27632. Inhibits the phosphorylation of MARCKS in cells stimulated by lysophosphatidic acid and inhibits EP3-stimulated NO formation. H-1152 . dihydrochloride prevents fragmentation of apoptotic cells. Relieves neuropathic pain.


References

1. Ikenoya, M., et al. 2002. J. Neurochem. 81: 9-16.
2. Sasaki, Y., et al. 2002. Pharmacol. Ther. 93: 225-232.
3. Sasaki, Y. 2003. J. Pharmacol. Sci. 93: 35-40.
4. Breitenlechner, C., et al. 2003. Structure. 11: 1595-1607.
5. Tatsumi, S., et al. 2005. Neuroscience. 131: 491-498.
6. Matsumura, S., et al. 2005. Biochem Biophys Res Commun. 338: 550-557.
7. Orlando, K.A., et al. 2006. Exp. Cell Res. 312: 5-15.
8. Zhang, Z., et al. 2006. Cell. Mol. Biol. Lett. 11: 12-29.
9. Pfitzer, G., et al. 2006. J. Muscle Res. Cell. Motil. 27: 445-454.
10. Breslin, J.W., et al. 2006. Am. J. Physiol. Heart Circ. Physiol. 290: H741-750.

Physical State :
Solid
Solubility :
Soluble in water, ethanol (~20 mg/ml), DMSO (~12.5 mg/ml), DMF (~15 mg/ml), and methanol.
Storage :
Store at -20° C
Melting Point :
182-184° C
Refractive Index :
n20D 1.59 (Predicted)
Optical Activity :
α20/D +18.8°, c = 1 in water
Ki Data :
ROCK: Ki= 1.6 nM; Y-27632: Ki= 140 nM; HA-1077: Ki= 330 nM; PKA: Ki= 630 nM; myosin light chain kinase: Ki= 10.1 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11560225
MDL Number :
MFCD06411451
SMILES :
CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)C.Cl.Cl

Download SDS (MSDS)

Certificate of Analysis

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H-1152 dihydrochloride (CAS 451462-58-1)  Product Citations

See how others have used H-1152 dihydrochloride (CAS 451462-58-1). Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 28102353  Wiggan, O. et al. 2017. Sci Rep. 7: 40953.

PMID: # 21821782  Morin, C. et al. 2011. Am. J. Physiol. Heart Circ. Physiol. 301: H1311-8.

PMID: # 31388001  Nat Commun. 10: 3529.

PMID: # 31292242  J. Virol. 93:

PMID: # 28486561  PLoS ONE. e0177046.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Kurtz Kurtz, KH. et al. (PubMed 24710574) used the Rho kinase inhibitor, H-1152 dihydrochloride, to find that Rho kinase enhances contractions of rat mesenteric collecting lymphatics. -SCBT Publication Review
Date published: 2015-01-23
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