Catalog No. size PriceQuantity
M6859-2 2mg solid $108
M6859-10 10mg solid $447


GSK180736A is potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM25 and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).

Product information

CAS Number: 817194-38-0

Molecular Weight: 365.36

Formula: C19H16FN5O2

Chemical Name: 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

Smiles: CC1NC(=O)NC(C=1C(=O)NC1C=C2C=NNC2=CC=1)C1C=CC(F)=CC=1


InChi: InChI=1S/C19H16FN5O2/c1-10-16(17(24-19(27)22-10)11-2-4-13(20)5-3-11)18(26)23-14-6-7-15-12(8-14)9-21-25-15/h2-9,17H,1H3,(H,21,25)(H,23,26)(H2,22,24,27)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM).


  1. Homan KT, Larimore KM, Elkins JM, Szklarz M, Knapp S, Tesmer JJ.Identification and structure-function analysis of subfamily selective Gprotein-coupled receptor kinase inhibitors. ACS Chem Biol. 2015 Jan16;10(1):310-9. doi: 10.1021/cb5006323. Epub 2014 Oct 3. PubMed PMID: 25238254; PubMed Central PMCID: PMC4301037.
  2. Homan KT, Waldschmidt HV, Glukhova A, Cannavo A, Song J, Cheung JY, Koch WJ, Larsen SD, Tesmer JJ. Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor. J Biol Chem. 2015 Aug21;290(34):20649-59. doi: 10.1074/jbc.M115.647370. Epub 2015 Jun 1. PubMed PMID: 26032411; PubMed Central PMCID: PMC4543626.
  3. Waldschmidt HV, Homan KT, Cruz-Rodriguez O, Cato MC, Waninger-Saroni J,Larimore KM, Cannavo A, Song J, Cheung JY, Kirchhoff PD, Koch WJ, Tesmer JJ,Larsen SD. Structure-Based Design, Synthesis and Biological Evaluation of HighlySelective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem.2016 Apr 6. [Epub ahead of print] PubMed PMID: 27050625.

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

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed