2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. GSK256066

GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.

For research use only. We do not sell to patients.

GSK256066 Chemical Structure

GSK256066 Chemical Structure

CAS No. : 801312-28-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 In-stock
Solution
10 mM * 1 mL in DMSO USD 108 In-stock
Solid
1 mg USD 32 In-stock
5 mg USD 95 In-stock
10 mg USD 160 In-stock
25 mg USD 320 In-stock
50 mg USD 520 In-stock
100 mg USD 840 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK256066:

GSK256066 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK256066

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease[1].

IC50 & Target[1]

PDE4

3.2 pM (IC50)

In Vitro

GSK256066 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1].
GSK256066 is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7[1].
GSK256066 inhibits PDE4 isoforms A-D with equal affinity (PDE4B: pIC50≥ 11.5, PDE4A: pIC50≥11.31, PDE4C: pIC50≥11.42, PDE4D: pIC50≥11.94)[1].
GSK256066 inhibits TNF-α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1].

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

GSK256066 Related Antibodies
In Vivo

GSK256066 (10 μg/kg; i.t.) causes significant inhibition of LPS-induced pulmonary neutrophilia[2].
GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED50=92 μg/kg)[2].
GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg)[2].

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

Animal Model: Male Brown Norway rats (180-200 g)[2]
Dosage: 10 μg/kg
Administration: Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge
Result: Inhibited the LPS-induced pulmonary neutrophilia.
Clinical Trial
Molecular Weight

518.58

Formula

C27H26N4O5S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N)C1=C(C2=CC(S(=O)(C3=CC=CC(C(N(C)C)=O)=C3)=O)=CC(C)=C2N=C1)NC4=CC=CC(OC)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (48.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9283 mL 9.6417 mL 19.2834 mL
5 mM 0.3857 mL 1.9283 mL 3.8567 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9283 mL 9.6417 mL 19.2834 mL 48.2086 mL
5 mM 0.3857 mL 1.9283 mL 3.8567 mL 9.6417 mL
10 mM 0.1928 mL 0.9642 mL 1.9283 mL 4.8209 mL
15 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2139 mL
20 mM 0.0964 mL 0.4821 mL 0.9642 mL 2.4104 mL
25 mM 0.0771 mL 0.3857 mL 0.7713 mL 1.9283 mL
30 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6070 mL
40 mM 0.0482 mL 0.2410 mL 0.4821 mL 1.2052 mL
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GSK256066 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK256066801312-28-7GSK 256066GSK-256066Phosphodiesterase (PDE)high-affinityphosphodiesterase4PDEPDE4BchronicobstructivepulmonarydiseaseInhibitorinhibitorinhibit

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