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GSK180736A

Catalog No. T3513 CAS 817194-38-0

Synonyms: GSK180736

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).

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GSK180736A, CAS 817194-38-0

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Purity: 98%

Biological Description

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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	ROCK1:100 nM, GRK2:0.77 μM
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].
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
Molecular Weight	365.368
Formula	C19H16FN5O2
CAS No.	817194-38-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 68 mg/mL (186.2 mM)

Ethanol: 3 mg/mL (8.21 mM)

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

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library GPCR Compound Library TGF-beta/Smad Compound Library Inhibitor Library DNA Damage & Repair Compound Library Neural Regeneration Compound Library Anti-Metabolism Disease Compound Library Cell Cycle Compound Library Fluorochemical Library Kinase Inhibitor Library

Related Products

Related compounds with same targets

GRK5-IN-2 1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID GSK180736A CCG215022 GSK299115A GSK270822A Takeda103A Paroxetine hydrochloride

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK180736A 817194-38-0 G蛋白偶联受体蛋白酪氨酸激酶干细胞细胞骨架细胞周期 GRK PKA ROCK inhibit Inhibitor ROK Rho-kinase Rho-associated kinase Rho-associated protein kinase GSK-180736A GSK180736 inhibitor

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