[CAS NO. 817194-38-0]  GSK180736A (GSK180736)

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PRODUCTS SPECIFICATIONS [817194-38-0]

Store
Catalog
SLK-S8489
Brand
Selleck
CAS
817194-38-0

DESCRIPTION [817194-38-0]

Overview

MDLMFCD30533616
Molecular Weight365.36
Molecular FormulaC19H16FN5O2
SMILESO=C(C1=C(C)NC(NC1C2=CC=C(F)C=C2)=O)NC3=CC4=C(NN=C4)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.7370 mL13.6851 mL27.3703 mL
5 mM0.5474 mL2.7370 mL5.4741 mL
10 mM0.2737 mL1.3685 mL2.7370 mL
50 mM0.0547 mL0.2737 mL0.5474 mL

Description

GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to 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 nM6.6(pIC50)

In vitro

GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).