H-1152 dihydrochloride

Cas：871543-07-6

Product Information：

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 Formula: C16H23Cl2N3O2S

Exact Mass: 391.0888

Molecular Weight: 392.34

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

Synonym:

H-1152 2HCl

Chemical Name:

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

InChi Key:

BFOPDSJOLUQULZ-UHFFFAOYSA-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

Smiles Code:

CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)C.Cl.Cl

Technical Data：

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

In Vitro：

H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC50s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively. H-1152 potently inhibits Rho kinase, with a Ki of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with Kis of 0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 µM) highly inhibits MARCKS phosphorylation, with an IC50 value of 2.5 µM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells. H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures.

References：

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

Products are for research use only. Not for human use.