(S)-H-1152 (hydrochloride)
Item № 10007653
CAS № 451462-58-1
Purity ≥95%
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL $0.00
500 µg $28.00 $0.00
1 mg $53.00 $0.00
5 mg $224.00 $0.00
10 mg $392.00 $0.00

Pricing updated 2016-05-24. Prices are subject to change without notice.

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Description

Rho-associated 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

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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 A crystalline solid
λmax 216, 280, 328 nm
SMILES CC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.Cl.Cl
InChI Code 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

WARNING - This product is not for human or veterinary use.

Shipping & Storage
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
Stability As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
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Additional Information

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References & Background Reading
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).

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