A ROCK inhibitor
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HA-1100 (hydrochloride)

Item No. 14413

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-1(2H)-isoquinolinone, monohydrochloride
CAS Number
155558-32-0
Molecular Formula
C14H17N3O3S • HCl
Formula Weight
343.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 1.1 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
246, 300 nm
SMILES
OC1=NC=CC2=C1C=CC=C2S(N3CCNCCC3)(=O)=O.Cl
InChi Code
InChI=1S/C14H17N3O3S.ClH/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17;/h1,3-5,7,15H,2,6,8-10H2,(H,16,18);1H
InChi Key
XWWFOUVDVJGNNG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $153

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    25 mg

    $336

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    Product Description

    HA-1100, a cell-permeable hydroxylated metabolite of HA-1077 (Item No. 10010559), is a potent inhibitor of Rho-associated kinase (ROCK) (Ki = 150 nM).1 It less effectively inhibits protein kinase A (Ki = 2.2 μM).1 It has been used to explore the role of ROCK in hypoxic and ischemic signaling as well as arterial relaxation.2,3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jacobs, M., Hayakawa, K., Swenson, L., et al. The structure of dimeric ROCK I reveals the mechanism for ligand selectivity. The Journal of Biological Chemisty 281(1), 260-268 (2006).

    2. Nakamura, K., Nishimura, J., Hirano, K., et al. Hydroxyfasudil, an active metabolite of fasudil hydrochloride, relaxes the rabbit basilar artery by disinhibition of myosin light chain phosphatase. J. Cereb. Blood Flow Metab. 21(7), 876-885 (2001).

    3. Takemoto, M., Sun, J., Hiroki, J., et al. Rho-kinase mediates hypoxia-induced downregulation of endothelial nitric oxide synthase. Circulation 106(1), 57-62 (2002).

    4. Wolfrum, S., Dendorfer, A., Rikitake, Y., et al. Inhibition of rho-kinase leads to rapid activation of phosphatidylinositol 3-kinase/protein kinase Akt and cardiovascular protection. Arterioscler. Thromb. Vasc. Biol. 24(10), 1842-1847 (2004).

    5. Satoh, S.i., Utsunomiya, T., Tsurui, K., et al. Pharmacological profile of hydroxy fasudil as a selective rho kinase inhibitor on ischemic brain damage. Life Sci. 69(12), 1441-1453 (2001).