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H 1152 dihydrochloride

Catalog #: 2414
16 Citations 3 Reviews Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
2414/1
H 1152 dihydrochloride | CAS No. 871543-07-6 | Rho-kinase Inhibitors
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Description: Selective Rho-kinase (ROCK) inhibitor

Chemical Name: (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride

Purity: ≥98%

Product Details
Citations (16)
Supplemental Products
Reviews (3)
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

H 1152 dihydrochloride is a rho-kinase (ROCK) inhibitor that displays high selectivity over other protein kinases (IC50 values are 0.012, 0.180, 0.360, 0.745, 3.03, 5.68 and 28.3 μM for ROCKII, CAMKII, PKG, Aurora A, PKA, PKC and MLCK respectively). Inhibits sulprostone-induced contractions in guinea pig aorta (IC50 = 190 nM) and displays proerectile effects in rats.

Glycyl Derivative also available.

Technical Data

M.Wt:
392.34
Formula:
C16H21N3O2S.2HCl
Solubility:
Soluble to 100 mM in water and to 50 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at +4°C
CAS No:
871543-07-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Other Product-Specific Information:

Background References

  1. ODZ1 allows glioblastoma to sustain invasiveness through a Myc-dependent transcriptional upregulation of RhoA

    Oncogene, 2016;0(0):.
  2. Roco kinase structures give insights into the mechanism of Parkinson disease-related leucine-rich-repeat kinase 2 mutations.

    Proc Natl Acad Sci U S A, 2012;109(26):10322-7.
  3. Dynamic blebbing: A bottleneck to human embryonic stem cell culture that can be overcome by Laminin-Integrin signaling
    NJ Weng, C Cheung, P Talbot
    Stem Cell Res, 2018;33(0):233-246.
  4. Influenza promotes collagen deposition via alphavbeta6 integrin-mediated transforming growth factor beta activation.
    Jolly L, Stavrou A, Vanderstoken G, Meliopoulos V, Habgood A, Tatler A, Porte J, Knox A, Weinreb P, Violette S, Hussell T, Kolb M, Stampfli M, Schultz-Cherry S, Jenkins G
    J Biol Chem, 2014;289(51):35246-63.
  5. Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells
    DTV Diep, K Hong, T Khun, M Zheng, A Ul-Haq, HS Jun, YB Kim, KH Chun
    Sci Rep, 2018;8(1):2477.
  6. Involvement of Rho-kinase in contraction of guinea-pig aorta induced by prostanoid EP3 receptor agonist.
    Shum et al.
    Br.J.Pharmacol., 2003;139:1449
  7. Proerectile effects of the rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine (H-1152) in the rat penis.
    Teixeira et al.
    J.Pharmacol.Exp.Ther., 2005;315:155
  8. Development of specific Rho-kinase inhibitors and their clinical application.
    Tamura et al.
    Biochim.Biophys.Acta, 2005;1754:245
  9. Hepatocytes Delete Regulatory T Cells by Enclysis, a CD4+ T Cell Engulfment Process
    SP Davies, GM Reynolds, AL Wilkinson, X Li, R Rose, M Leekha, YS Liu, R Gandhi, E Buckroyd, J Grove, NM Barnes, RC May, SG Hubscher, DH Adams, Y Huang, O Qureshi, Z Stamataki
    Cell Rep, 2019;29(6):1610-1620.e4.

Product Datasheets

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Citations for H 1152 dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for H 1152 dihydrochloride include:

16 Citations: Showing 1 - 10

  1. Tissue curvature and apicobasal mechanical tension imbalance instruct cancer morphogenesis.
    Authors: Messal Et al.
    Nature  2019;566:126
  2. Rebalancing of actomyosin contractility enables mammary tumor formation upon loss of E-cadherin.
    Authors: Schipper Et al.
    Nat Commun  2019;10:3800
  3. Sp1-regulated expression of p11 contributes to motor neuron degeneration by membrane insertion of TASK1.
    Authors: García-Morales Et al.
    Nat Commun  2019;10:3784
  4. Rho-Kinase Inhibition Reduces Myofibroblast Differentiation and Proliferation of Scleral Fibroblasts Induced by Transforming Growth Factor β and Experimental Glaucoma.
    Authors: Pitha Et al.
    Transl Vis Sci Technol  2018;7:6
  5. Rho Kinase Inhibition by AT13148 Blocks Pancreatic Ductal Adenocarcinoma Invasion and Tumor Growth.
    Authors: Rath Et al.
    Cancer Res  2018;78:3321
  6. Expanding Actin Rings Zipper the Mouse Embryo for Blastocyst Formation.
    Authors: Zenker Et al.
    Cell  2018;173:776
  7. ROCK signaling promotes collagen remodeling to facilitate invasive pancreatic ductal adenocarcinoma tumor cell growth.
    Authors: Rath Et al.
    EMBO Mol Med  2017;9:198
  8. Oncogenic PIK3CA induces centrosome amplification and tolerance to genome doubling.
    Authors: Berenjeno Et al.
    Nat Commun  2017;8:1773
  9. Multiparametric Analysis of Cell Shape Demonstrates that β-PIX Directly Couples YAP Activation to Extracellular Matrix Adhesion.
    Authors: Sero and Bakal
    Cell Syst  2017;4:84
  10. RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6.
    Authors: Durkin Et al.
    Dev Cell  2017;41:315

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Reviews for H 1152 dihydrochloride

Average Rating: 4.7 (Based on 3 Reviews)

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In vitro study
By Anonymous on 06/25/2021
Species: Human

Different Concentration were tested in vitro and lysates were collected.

In vitro
By Anonymous on 02/28/2021
Species: Human

Dihydrochloride were added at different time points to collect RNA and lysates

In Vitro studay
By Anonymous on 02/08/2019
Species: Human

DMSO, 1uM and 10 μM H1152 dihydrochloride were added to cells for 24h for western.

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