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Chemical Structure| 871543-07-6 Chemical Structure| 871543-07-6

Structure of H-1152 2HCl
CAS No.: 871543-07-6

Chemical Structure| 871543-07-6

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H-1152 2HCl, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.

Synonyms: H-1152 dihydrochloride

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Product Details of H-1152 2HCl

CAS No. :871543-07-6
Formula : C16H23Cl2N3O2S
M.W : 392.34
SMILES Code : CC1=CN=CC2=C1C(S(=O)(N3[C@@H](C)CNCCC3)=O)=CC=C2.[H]Cl.[H]Cl
Synonyms :
H-1152 dihydrochloride
MDL No. :MFCD06411451

Safety of H-1152 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of H-1152 2HCl

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • ROCK2

    ROCK2, IC50:0.0120 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-468 cells 1 μM 24 hours inhibited TEAD reporter activity and cell proliferation Nat Commun. 2022 Feb 4;13(1):703
MCF10A cells 1 μM 24 hours inhibited TEAD reporter activity Nat Commun. 2022 Feb 4;13(1):703
PC-12 cells 10 µM 24 hours Induced neurite outgrowth, formed fully extended neurites Cell Mol Biol Lett. 2006;11(1):12-29
MDA-MB-231 cells 1 μM 24 hours inhibited TEAD reporter activity and cell proliferation Nat Commun. 2022 Feb 4;13(1):703
H2373 cells 1 μM 24 hours inhibited TEAD reporter activity and cell proliferation Nat Commun. 2022 Feb 4;13(1):703
human umbilical vein endothelial cells (HUVECs) 3 µM 30 minutes Inhibited ROCK activity, reversed CCM2 siRNA-induced MLC phosphorylation and stress fiber formation, and reduced monolayer permeability J Exp Med. 2010 Apr 12;207(4):881-96
human umbilical vein endothelial cells (HUVECs) 3 µM 30 minutes Inhibited ROCK activity, reversed KRIT1 siRNA-induced MLC phosphorylation and stress fiber formation, and reduced monolayer permeability J Exp Med. 2010 Apr 12;207(4):881-96
coronary arterioles 10^-8 M 60 minutes H-1152 alleviated oxidative stress and abolished enhanced vasoconstriction to ET-1 by inhibiting the ROCK signaling pathway. Cardiovasc Res. 2017 Sep 1;113(11):1329-1337
PC-12 cells 1 µM 5-30 minutes Induced neurite outgrowth, observed rapid cell shape change and neurite formation Cell Mol Biol Lett. 2006;11(1):12-29
human dermal microvascular endothelial cells (HMVECs) 20 μmol/L 0.5 hours H-1152 attenuated the AGE-induced alteration in monolayer permeability and cytoskeleton Cardiovasc Diabetol. 2012 Jan 17;11:7
INSw/GFPHES3 cells 10 μM 8 days Promote the generation and maturation of beta-like cells in three-dimensional culture, H1152 treatment significantly increases the percentage of INS+ cells and the expression of mature beta cell markers Nat Commun. 2017 Aug 21;8(1):298
HUES8 cells 10 μM or 1 μM 4 days Promote the generation of insulin-expressing cells from pancreatic progenitors, H1152 treatment significantly increases the percentage of INS+ cells Nat Commun. 2017 Aug 21;8(1):298
TKCC5 human PDAC cells 10 µM 1 hour Inhibited ROCK substrate phosphorylation, reduced phosphorylation of MLC2 and MYPT1 Cancer Res. 2018 Jun 15;78(12):3321-3336
KPC mouse PDAC cells 10 µM 1 hour Inhibited ROCK substrate phosphorylation, reduced phosphorylation of MLC2 and MYPT1 Cancer Res. 2018 Jun 15;78(12):3321-3336
hippocampal neurons 100 nM 60 minutes blocking the RhoA effector ROCK to prevent CRH-induced loss of thin dendritic spines Mol Psychiatry. 2013 Apr;18(4):485-96

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID mice Breast tumor xenograft model Intraperitoneal injection 25 mg/kg Once daily for 31 days Inhibited tumor growth Nat Commun. 2022 Feb 4;13(1):703
SCID-beige mice Diabetes model Subrenal capsule transplantation 10 μM Single transplantation, observed up to 4.5 months post-transplantation Evaluate the function of H1152-treated beta-like cells in vivo, results show that H1152-treated cells have improved capacities to respond to glucose stimulation and maintain glucose homeostasis Nat Commun. 2017 Aug 21;8(1):298

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.49mL

5.10mL

2.55mL

References

 

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