Home GPCR & G Protein GRK inhibitor GSK180736A (GSK180736) For research use only.

GSK180736A (GSK180736)

GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.

GSK180736A (GSK180736) Chemical Structure

GSK180736A (GSK180736) Chemical Structure

CAS No. 817194-38-0

Purity & Quality Control

Batch: S848901 DMSO]73 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.23%
99.23

GSK180736A (GSK180736) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Function assay Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA, IC50=0.014 μM 18842034
Sf9 cells Function assay 10 mM Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM, IC50=0.014 μM 17201405
Click to View More Cell Line Experimental Data

Biological Activity

Description GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.
Targets
ROCK [3]
(Cell-free assay)		 GRK2 [1]
(Cell-free assay)
100 nM 6.6(pIC50)
In vitro
In vitro GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5[2]. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM)[3].

Chemical Information & Solubility

Molecular Weight 365.36 Formula

C19H16FN5O2
CAS No. 817194-38-0 SDF Download GSK180736A (GSK180736) SDF
Smiles CC1=C(C(NC(=O)N1)C2=CC=C(C=C2)F)C(=O)NC3=CC4=C(C=C3)NN=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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