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

Item No. 13332

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-amino-1-[(3S)-hexahydro-3-methyl-4-[(4-methyl-5-isoquinolinyl)sulfonyl]-1H-1,4-diazepin-1-yl]-ethanone, dihydrochloride
CAS Number
913844-45-8
Synonyms
  • Rho Kinase Inhibitor IV
Molecular Formula
C18H24N4O3S • 2HCl
Formula Weight
449.4
Purity
≥98%
Formulation (Request formulation change)
A 5 mg/ml solution in methanol
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
216, 280, 328 nm
SMILES
O=S(C1=CC=CC2=C1C(C)=CN=C2)(N3CCCN(C(CN)=O)C[C@@H]3C)=O
InChi Code
InChI=1S/C18H24N4O3S/c1-13-10-20-11-15-5-3-6-16(18(13)15)26(24,25)22-8-4-7-21(12-14(22)2)17(23)9-19/h3,5-6,10-11,14H,4,7-9,12,19H2,1-2H3/t14-/m0/s1
InChi Key
CMKMGFAUKPAOMG-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $103

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    1 mg

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    Product Description

    Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK2).1 It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥10 μM for each).1 The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tamura, M., Nakao, H., Yoshizaki, H., et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim. Biophys. Acta 1754(1-2), 245-252 (2005).

    2. Ishizaki, T., Uehata, M., Tamechika, I., et al. Pharmacological properties of Y-27632, a specific inhibitor of Rho-associated kinases. Mol. Pharmacol. 57(5), 976-983 (2000).