Free shipping on all orders over $ 500

H-1152

Cat. No. M4938
H-1152 Structure
Size Price Availability
2mg USD 125  USD125 Out of stock
5mg USD 185  USD185 Out of stock
10mg USD 325  USD325 Out of stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

H-1152 dose-dependently inhibited the phosphorylation of MARCKS in human neuroteratoma (NT-2) cells stimulated by Rho-activator lysophosphatidic acid (LPA), which was determined by phosphorylation site-specific antibody against phospho-Ser159 in MARCKS, whereas it hardly inhibited the phosphorylation stimulated by phorbol-12,13-dibutyrate (PDBu).Loss-of-function experiments in endothelial cells revealed that inhibition of ROCK I/II using the pharmacological inhibitor H-1152 and ROCK I/II-specific small-interfering RNAs resulted in a rise of VEGF-driven sprouting angiogenesis.

Product Citations
Chemical Information
Molecular Weight 319.42
Formula C16H21N3O2S
CAS Number 451462-58-1
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ikenoya M,et.al. J Neurochem. 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.

Related ROCK Products
Akt/ROCK-IN-1

Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively.

Scaff10-8

Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation.

ROCK-IN-6

ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM.

ROCK-IN-4

ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability.

ROCK-IN-32

ROCK-IN-32 is a ROCK inhibitor, with an IC50 value of 11 nM for ROCK2.

  Catalog
Abmole Inhibitor Catalog




Keywords: H-1152 supplier, ROCK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.