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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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G288221-10mg
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10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$173.90
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G288221-50mg
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50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$543.90
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|
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G288221-100mg
|
100mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$924.90
|
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β-TrCP1 ligase inhibitor
| Synonyms | 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid |
|---|---|
| Specifications & Purity | ≥98%(HPLC) |
| Biochemical and Physiological Mechanisms | β-TrCP1 ligase inhibitor. Inhibits IκBαubiquitination (IC50= 5.2μM) without affecting proteasome activity. Blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. Suppresses antigen-induced NFκB expression, inflammation and |
| Storage Temp | Store at 2-8°C |
| Shipped In |
Wet ice This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
GS143 is a selective inhibitor of IκBα ubiquitination with IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes. GS143 exhibits anti-asthma effect. |
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Class | Benzene and substituted derivatives |
| Subclass | Benzoic acids and derivatives |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Acylaminobenzoic acid and derivatives |
| Alternative Parents | Benzoic acids Benzoyl derivatives Fluorobenzenes Pyrazolones Aryl fluorides Heteroaromatic compounds Furans Oxacyclic compounds Monocarboxylic acids and derivatives Carboxylic acids Azacyclic compounds Organopnictogen compounds Organonitrogen compounds Organofluorides Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Acylaminobenzoic acid or derivatives - Benzoic acid - Benzoyl - Halobenzene - Fluorobenzene - Pyrazolinone - Aryl halide - Aryl fluoride - Heteroaromatic compound - Pyrazoline - Furan - Oxacycle - Azacycle - Organoheterocyclic compound - Monocarboxylic acid or derivatives - Carboxylic acid - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Carbonyl group - Aromatic heteromonocyclic compound |
| Description | This compound belongs to the class of organic compounds known as acylaminobenzoic acid and derivatives. These are derivatives of amino benzoic acid derivatives where the amine group is N-acylated. |
| External Descriptors | Not available |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| IUPAC Name | 4-[(4E)-3-benzyl-4-[[5-(2-fluorophenyl)furan-2-yl]methylidene]-5-oxopyrazol-1-yl]benzoic acid |
|---|---|
| INCHI | InChI=1S/C28H19FN2O4/c29-24-9-5-4-8-22(24)26-15-14-21(35-26)17-23-25(16-18-6-2-1-3-7-18)30-31(27(23)32)20-12-10-19(11-13-20)28(33)34/h1-15,17H,16H2,(H,33,34)/b23-17+ |
| InChIKey | IZPMWFSVTDOCDI-HAVVHWLPSA-N |
| Smiles | C1=CC=C(C=C1)CC2=NN(C(=O)C2=CC3=CC=C(O3)C4=CC=CC=C4F)C5=CC=C(C=C5)C(=O)O |
| Isomeric SMILES | C1=CC=C(C=C1)CC\2=NN(C(=O)/C2=C/C3=CC=C(O3)C4=CC=CC=C4F)C5=CC=C(C=C5)C(=O)O |
| Molecular Weight | 466.46 |
| Reaxy-Rn | 13103224 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13103224&ln= |
| Solubility | Solvent:DMSO, Max Conc. mg/mL: 46.65, Max Conc. mM: 100 |
|---|---|
| Molecular Weight | 466.500 g/mol |
| XLogP3 | 5.400 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 6 |
| Exact Mass | 466.133 Da |
| Monoisotopic Mass | 466.133 Da |
| Topological Polar Surface Area | 83.100 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 844.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 1 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 1 |
| Covalently-Bonded Unit Count | 1 |