A ROCK inhibitor
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(S)-H-1152 (hydrochloride)

Item No. 10007653

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-methyl-isoquinoline, dihydrochloride
CAS Number
451462-58-1
Molecular Formula
C16H21N3O2S • 2HCl
Formula Weight
392.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 12.5 mg/mlEthanol: 20 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
216, 280, 328 nm
SMILES
CC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.Cl.Cl
InChi Code
InChI=1S/C16H21N3O2S.2ClH/c1-12-9-18-11-14-5-3-6-15(16(12)14)22(20,21)19-8-4-7-17-10-13(19)2;;/h3,5-6,9,11,13,17H,4,7-8,10H2,1-2H3;2*1H/t13-;;/m0../s1
InChi Key
BFOPDSJOLUQULZ-GXKRWWSZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    Product Description

    H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM).12 It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM).2 H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 μM, respectively).2 It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly,3 vasoconstriction,4 as well as spontaneously tonic smooth muscle5 and neurite extension.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sasaki, Y., Suzuki, M., and Hidaka, H. The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway. Pharmacol. Ther. 93, 225-232 (2002).

    2. Ikenoya, M., Hidaka, H., Hosoya, T., 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. 81, 9-16 (2002).

    3. Davies, S.L., Gibbons, C.E., Vizard, T., et al. Ca2+-sensing receptor induces Rho kinase-mediated actin stress fiber assembly and altered cell morphology, but not in response to aromatic amino acids. Am. J. Physiol. Cell Physiol. 290, C1543-C1551 (2006).

    4. Johnson, R.P., El-Yazbi, A.F., Takeya, K., et al. Ca2+ sensitization via phosphorylation of myosin phosphatase targeting subunit at threonine-855 by Rho kinase contributes to the arterial myogenic response. J. Physiol. 587(11), 2537-2553 (2009).

    5. Rattan, S., and Patel, C.A. Selectivity of Rho kinase (ROCK) inhibitors in the spontaneously tonic smooth muscle. Am. J. Physiol. Gastrointest. Liver Physiol. 294(3), G687-G693 (2008).

    6. Fuentes, E.O., Leemhuis, J., Stark, G.B., et al. Rho kinase inhibitors Y27632 and H1152 augment neurite extension in the presence of cultured Schwann cells. J. Brachial Plex. Peripher. Nerve Inj. 3(19), (2008).