H-1152 dihydrochloride | CAS# 871543-07-6 | ROCK inhibitor

MedKoo Cat#: 574726 | Name: H-1152 dihydrochloride

Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

H-1152 dihydrochloride is an isoquinolinesulfonamide derivative that is a membrane-permeable inhibitor of Rho-kinase but poor inhibitor of other serine/threonine kinases.

Chemical Structure

H-1152 dihydrochloride

CAS#871543-07-6 (2HCl)

Theoretical Analysis

MedKoo Cat#: 574726

Name: H-1152 dihydrochloride

CAS#: 871543-07-6 (2HCl)

Chemical Formula: C16H23Cl2N3O2S

Exact Mass: 0.0000

Molecular Weight: 392.34

Elemental Analysis: C, 48.98; H, 5.91; Cl, 18.07; N, 10.71; O, 8.16; S, 8.17

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 650.00	2 Weeks
50mg	USD 950.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

451462-58-1 (free base) 871543-07-6 (2HCl)

Synonym

H-1152 dihydrochloride; H-1152 2HCl; H-1152 HCl; H1152 HCl; H 1152 HCl;

IUPAC/Chemical Name

(S)-4-methyl-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline dihydrochloride

InChi Key

BFOPDSJOLUQULZ-GXKRWWSZSA-N

InChi Code

InChI=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

SMILES Code

CC1=CN=CC2=C1C(S(=O)(N3[C@H](CNCCC3)C)=O)=CC=C2.[H]Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.

In vitro activity:

The selective ROCK inhibitor H1152 was applied to THP-1 cells before the induction of differentiation by PMA, and the phosphorylation of MYPT1 was tested after 48 h. H1152 treatment not only decreased the basal level of MYPT1 phosphorylation in non-differentiated cells (although this tendency of changes was not significant), but it also prevented partially the PMA-induced increase in both MYPT1pThr696 and MYPT1pThr853 levels (Figure 3A). Reference: Int J Mol Sci. 2021 Mar 3;22(5):2516. https://pubmed.ncbi.nlm.nih.gov/33802280/

In vivo activity:

Compared with the rabbit corneas treated with balanced saline solution, the H-1152–treated ones exhibited areas of wound closure, as well as multinucleate CECs with variable morphology suggestive of enhanced migration and proliferation associated with wound healing (Fig. 7). Reference: Invest Ophthalmol Vis Sci. 2016 Dec 1;57(15):6731-6738. https://pubmed.ncbi.nlm.nih.gov/27951595/

	Solvent	mg/mL	mM
Solubility
	Water	37.5	95.50

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 392.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Tóth E, Erdődi F, Kiss A. Myosin Phosphatase Is Implicated in the Control of THP-1 Monocyte to Macrophage Differentiation. Int J Mol Sci. 2021 Mar 3;22(5):2516. doi: 10.3390/ijms22052516. PMID: 33802280; PMCID: PMC7959147. 2. Ikenoya M, Hidaka H, Hosoya T, Suzuki M, Yamamoto N, Sasaki Y. 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. 2002 Apr;81(1):9-16. doi: 10.1046/j.1471-4159.2002.00801.x. PMID: 12067241.

In vitro protocol:

In vivo protocol:

1. Chen YL, Ren Y, Xu W, Rosa RH Jr, Kuo L, Hein TW. Constriction of Retinal Venules to Endothelin-1: Obligatory Roles of ETA Receptors, Extracellular Calcium Entry, and Rho Kinase. Invest Ophthalmol Vis Sci. 2018 Oct 1;59(12):5167-5175. doi: 10.1167/iovs.18-25369. PMID: 30372743; PMCID: PMC6203175. 2. Meekins LC, Rosado-Adames N, Maddala R, Zhao JJ, Rao PV, Afshari NA. Corneal Endothelial Cell Migration and Proliferation Enhanced by Rho Kinase (ROCK) Inhibitors in In Vitro and In Vivo Models. Invest Ophthalmol Vis Sci. 2016 Dec 1;57(15):6731-6738. doi: 10.1167/iovs.16-20414. PMID: 27951595; PMCID: PMC6018452.

1. Lie M, Grover M, Whitlon DS. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010;169(2):855-862. doi:10.1016/j.neuroscience.2010.05.020