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GPCR/G Protein GRK GSK180736A

GSK180736A

Catalog No. T3513   CAS 817194-38-0
Synonyms: GSK180736
Purity 98.44% Datasheet

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

GSK180736A, CAS 817194-38-0
Pack Size Availability Price/USD Quantity
2 mg In stock 60.00
5 mg In stock 75.00
10 mg In stock 101.00
25 mg In stock 200.00
50 mg In stock 360.00
100 mg In stock 665.00
1 mL * 10 mM (in DMSO) In stock 75.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
Targets&IC50 GRK1 :ic50 <3(pIC50),   GRK2 :ic50 6.6(pIC50),   GRK5 :ic50 4(pIC50),   PKA :ic50 30μM,   ROCK :ic50 100nM,  
Cell Research
Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1].
Synonyms GSK180736
Purity 98.44%
Appearance solid
Molecular Weight 365.13
Formula C19H16FN5O2
CAS No. 817194-38-0

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 68 mg/mL (186.2 mM)

Ethanol: 3 mg/mL (8.21 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Homan KT, et al. ACS Chem Biol. 2015, 10(1):310-9. 2. Homan KT, et al. J Biol Chem. 2015, 290(34):20649-59. 3. Helen V. Waldschmidt, et al. J Med Chem. 2016, 59 (8):3793-3807. 4. Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library Stem cell Differentiation Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library GPCR Compound Library Fluorochemical Library TGF-beta/Smad Compound Library Cell cycle related Compound Library

Related Products

Related compounds with same targets
Paroxetine hydrochloride CCG215022 GSK180736A Ellagic acid Piceatannol Bucladesine sodium salt BX912 Theophylline-7-acetic acid

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