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Cayman is a manufacturer, supplier, and vendor of biochemical reagents, assay kits, forensic chemistry standards, antibodies, and proteins for scientific research. Analytical testing services and custom synthesis are also available.

Cayman Chemical Company · 1180 East Ellsworth Road · Ann Arbor, Michigan 48108 · USA

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(S)-H-1152 (hydrochloride)

Cayman Chemical Item Number 10007653

(CAS 451462-58-1)

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Rho kinase (ROCK), activated by GTP-linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. 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

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).

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
Formulation A crystalline solid
Purity ≥95%
λmax 216, 280, 328 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
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(S)-H-1152 (hydrochloride) is available in the following screening library:

Size Price Quantity Subtotal
500 µg $28.00 $0.00
1 mg $53.00 $0.00
5 mg $224.00 $0.00
10 mg $392.00 $0.00
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Cart Total $0.00

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Pricing updated 2015-02-27. Prices are subject to change without notice.

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Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.

Upon receipt, it is important to check the storage requirements of your products and place them at the appropriate temperature. Products shipped without ice may require frozen storage for long term stability.

Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.

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