GSK-180736A( GSK 180736A | GSK180736A )

Catalog No. M16042 CAS No. 817194-38-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK-180736A
Note

Research use only, not for human use.
Brief Description

A highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM.
Description

A highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM; displays >400-fold selective for GRK2 over both GRK1 and GRK5, with no inhibition on PKA; also inhibits ROCK with IC50 of 0.1 uM.
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).
In Vivo

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Synonyms

GSK 180736A | GSK180736A
Pathway

Others
Target

GRK (GPCRK)
Recptor

GRK1|GRK2|GRK5|PKA|ROCK
Research Area

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Indication

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CAS Number

817194-38-0
Formula Weight

365.3611
Molecular Formula

C19H16FN5O2
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 30 mg/mL
SMILES

CC1=C(C(NC(=O)N1)C2=CC=C(C=C2)F)C(=O)NC3=CC4=C(C=C3)NN=C4
Chemical Name

5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-

1. Homan KT, et al. ACS Chem Biol. 2015 Jan 16;10(1):310-9. 2. Waldschmidt HV, et al. J Med Chem. 2016 Apr 28;59(8):3793-807.

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