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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P334165-5mg | 5mg | In stock | $474.90 | |
P334165-10mg | 10mg | In stock | $785.90 | |
P334165-25mg | 25mg | In stock | $1,654.90 | |
P334165-50mg | 50mg | In stock | $2,646.90 | |
P334165-100mg | 100mg | In stock | $4,342.90 |
a cell-permeable allosteric inhibitor of the PTP1B (protein tyrosine phosphatase 1B) enzyme.
Specifications & Purity | ≥95% |
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Biochemical and Physiological Mechanisms | Cell permeable: yes Target IC50: 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively Product does not compete with ATP. Primary Target PTP1B403 Reversible: yes |
Storage Temp | Protected from light,Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | PTP1B Inhibitor blocks the activity of the Protein Tyrosine Phosphatase 1B, which is a key factor in the negative regulation of insulin and leptin signaling pathway. Molecular dynamic studies have shown that PTP1B Inhibitor has strong binding and high selectivity due to the hydrogen bonding networks formed around the active sites. Cytotoxicity and low revival rates throughout clone generation and maintence result if PTP1B is over-expressed in CHO and HEK293 stable cell clones. Studies have shown that PTP1B Inhibitor could dramatically magnify the membrane translocation of the key glucose transporter Glut4 in PTP1B-overexpressed CHO cells. PTP1B Inhibitor selectively increases the phosphorylation of the insulin receptor, insulin receptor substrate 1, and Akt, mimicking the action of insulin. PTP1B Inhibitor is also known as Protein Tyrosine Phosphatase 1B Inhibitor, and 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]-6-benzofuransulfonamide. |
pKa | pKa: 4.47 (Predicted), pKa: 1.70 (Predicted) |
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IUPAC Name | 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide |
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INCHI | InChI=1S/C26H19Br2N3O7S3/c1-2-21-23(24(32)14-11-19(27)25(33)20(28)12-14)18-8-7-17(13-22(18)38-21)41(36,37)30-15-3-5-16(6-4-15)40(34,35)31-26-29-9-10-39-26/h3-13,30,33H,2H2,1H3,(H,29,31) |
InChi Key | SXKBTDJJEQQEGE-UHFFFAOYSA-N |
Canonical SMILES | CCC1=C(C2=C(O1)C=C(C=C2)S(=O)(=O)NC3=CC=C(C=C3)S(=O)(=O)NC4=NC=CS4)C(=O)C5=CC(=C(C(=C5)Br)O)Br |
Isomeric SMILES | CCC1=C(C2=C(O1)C=C(C=C2)S(=O)(=O)NC3=CC=C(C=C3)S(=O)(=O)NC4=NC=CS4)C(=O)C5=CC(=C(C(=C5)Br)O)Br |
PubChem CID | 448662 |
Molecular Weight | 741.45 |
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Lot Number | Certificate Type | Date | Item |
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B2303671 | Certificate of Analysis | Jan 03, 2023 | P334165 |
B2313520 | Certificate of Analysis | Jan 03, 2023 | P334165 |
B2313614 | Certificate of Analysis | Jan 03, 2023 | P334165 |
B2313648 | Certificate of Analysis | Jan 03, 2023 | P334165 |
B2313659 | Certificate of Analysis | Jan 03, 2023 | P334165 |
Solubility | Soluble in DMSO, and ethanol. |
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Sensitivity | light sensitive |
Refractive Index | n20D1.73 |
Boil Point(°C) | 855° C at 760 mmHg |