1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK

GSK180736A 

Cat. No.: HY-18990 Purity: 98.05%
Handling Instructions

GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

For research use only. We do not sell to patients.
GSK180736A Chemical Structure

GSK180736A Chemical Structure

CAS No. : 817194-38-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 87 In-stock
2 mg USD 72 In-stock
5 mg USD 108 In-stock
10 mg USD 144 In-stock
50 mg USD 480 In-stock
100 mg USD 900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

IC50 & Target

IC50: 0.77 μM (GRK2), 100 nM (ROCK1)[1]

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.7370 mL 13.6851 mL 27.3703 mL
5 mM 0.5474 mL 2.7370 mL 5.4741 mL
10 mM 0.2737 mL 1.3685 mL 2.7370 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

365.36

Formula

C₁₉H₁₆FN₅O₂

CAS No.

817194-38-0

SMILES

CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC=C(F)C=C4)NC1=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
GSK180736A
Cat. No.:
HY-18990
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