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GSK256066 - ≥98%, high purity , Phosphodiesterase 4 inhibitor, CAS No.801312-28-7, Phosphodiesterase 4 inhibitor

COA COA
In stock
Item Number
G127379
Grouped product items
SKU Size
Availability
 Price Qty
G127379-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$25.90
G127379-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$72.90
G127379-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$335.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet
View related series
Metabolic Enzyme/Protease (4860) Nucleic Acid Metabolism (395) Phosphodiesterase (PDE) (252)

Basic Description

Synonyms DTXSID30230090 | AC-32928 | Histidine-Alanine dipeptide | MFCD18206923 | MLS006011116 | 6-[3-(Dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide | SMR004702897 | NCGC00346620-06 | C27H26N4O5S | NCGC00346620-08 | SCHEMBL
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of
Storage Temp Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Phosphodiesterase 4 inhibitor
Product Description

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7
A highly potent and selective inhibitor of phosphodiesterase 4

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Quinolines and derivatives
Subclass Quinoline carboxamides
Intermediate Tree Nodes Not available
Direct Parent Quinoline-3-carboxamides
Alternative Parents 4-aminoquinolines  Aminophenyl ethers  Pyridinecarboxylic acids and derivatives  Benzamides  Benzenesulfonyl compounds  Methoxyanilines  Anisoles  Phenoxy compounds  Methoxybenzenes  Benzoyl derivatives  Alkyl aryl ethers  Aminopyridines and derivatives  Primary aromatic amines  Vinylogous amides  Sulfones  Tertiary carboxylic acid amides  Heteroaromatic compounds  Primary carboxylic acid amides  Amino acids and derivatives  Azacyclic compounds  Secondary amines  Hydrocarbon derivatives  Organic oxides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Quinoline-3-carboxamide - Aminoquinoline - 4-aminoquinoline - Pyridine carboxylic acid or derivatives - Methoxyaniline - Benzoic acid or derivatives - Benzamide - Benzenesulfonyl group - Aminophenyl ether - Benzoyl - Aniline or substituted anilines - Anisole - Phenol ether - Phenoxy compound - Methoxybenzene - Alkyl aryl ether - Aminopyridine - Monocyclic benzene moiety - Benzenoid - Primary aromatic amine - Pyridine - Tertiary carboxylic acid amide - Sulfonyl - Sulfone - Heteroaromatic compound - Vinylogous amide - Primary carboxylic acid amide - Amino acid or derivatives - Carboxamide group - Secondary amine - Ether - Carboxylic acid derivative - Azacycle - Amine - Organic nitrogen compound - Organonitrogen compound - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Organooxygen compound - Organosulfur compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as quinoline-3-carboxamides. These are quinolines in which the quinoline ring system is substituted by one carboxamide group at the 3-position.
External Descriptors Not available

Associated Targets(Human)

PDE4B Tclin Phosphodiesterase 4B (2748 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Homo sapiens (32628 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PBMC (10003 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDE4A Tclin Phosphodiesterase 4 (3344 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Blood (6 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Lung (9 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsome (341 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Whole blood (71 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide
INCHI InChI=1S/C27H26N4O5S/c1-16-11-21(37(34,35)20-10-5-7-17(12-20)27(33)31(2)3)14-22-24(16)29-15-23(26(28)32)25(22)30-18-8-6-9-19(13-18)36-4/h5-15H,1-4H3,(H2,28,32)(H,29,30)
InChIKey JFHROPTYMMSOLG-UHFFFAOYSA-N
Smiles CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C
Isomeric SMILES CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C
Molecular Weight 518.58
Reaxy-Rn 12158339
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12158339&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility：DMSO
Sensitivity Light sensitive
Molecular Weight 518.600 g/mol
XLogP3 3.800
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 7
Exact Mass 518.162 Da
Monoisotopic Mass 518.162 Da
Topological Polar Surface Area 140.000 Ų
Heavy Atom Count 37
Formal Charge 0
Complexity 922.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Alternative Products

  1. GSK256066, Phosphodiesterase 4 inhibitor
    GSK256066, Phosphodiesterase 4 inhibitor
    • 10mM in DMSO

    Starting at $82.90

Solution Calculators

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