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(S)-Glycyl-H-1152 (hydrochloride) Exclusive

Cayman Chemical Item Number 13332

Rho Kinase Inhibitor IV (CAS 913844-45-8)

(S)-Glycyl-H-1152 (hydrochloride) (CAS 913844-45-8)

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Description

Two Rho kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The Rho kinases play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal.123 Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II).4 It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits calcium/calmodulin kinase 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).4 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).4,5

1 Olson, M.F. Applications for ROCK kinase inhibition. Curr Opin Cell Biol 20 242-248 (2008).

2 Narumiya, S., Tanji, M., and Ishizaki, T. Rho signaling, ROCK and mDia1, in transformation, metastasis and invasion. Cancer Metastasis Rev 28 65-76 (2009).

3 Watanabe, K., Ueno, M., Kamiya, D., et al. A ROCK inhibitor permits survival of dissociated human embryonic stem cells. Nat Biotech 25(6) 681-686 (2007).

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

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

Synonyms
  • Rho Kinase Inhibitor IV
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
Molecular Formula C18H24N4O3S · 2HCl
Formula Weight 449.4
Formulation A solution in methanol
Purity ≥98%
λmax 216, 280, 328 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=S(C1=CC=CC2=C1C(C)​=CN=C2)​(N3CCCN(C(CN)​=O)​C[C@@H]​3C)​=O

Background Reading

Olson, M.F. Applications for ROCK kinase inhibition. Curr Opin Cell Biol 20 242-248 (2008).

Narumiya, S., Tanji, M., and Ishizaki, T. Rho signaling, ROCK and mDia1, in transformation, metastasis and invasion. Cancer Metastasis Rev 28 65-76 (2009).

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

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

Watanabe, K., Ueno, M., Kamiya, D., et al. A ROCK inhibitor permits survival of dissociated human embryonic stem cells. Nat Biotech 25(6) 681-686 (2007).

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Size Price Quantity Subtotal
500 µg $75.00 $0.00
1 mg $143.00 $0.00
5 mg $600.00 $0.00
10 mg $1,050.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

Related Products

CAY10622 Exclusive
HA-1077 (hydrochloride)
(S)-H-1152 (hydrochloride)
Y-27632 (hydrochloride)
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