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Key Documents

539741

Sigma-Aldrich

PTP1B Inhibitor

PTP1B Inhibitor, CAS 765317-72-4, is a cell-permeable, selective, reversible and non-competitive allosteric inhibitor of PTP1B (IC₅₀ = 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively).

Synonyme(s) :

PTP1B Inhibitor, 3-(3,5-Dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonicacid-(4-(thiazol-2-ylsulfamyl)-phenyl)-amide, PTP Inhibitor XXII

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About This Item

Formule empirique (notation de Hill):
C26H19Br2N3O7S3
Numéro CAS:
765317-72-4
Poids moléculaire :
741.45
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥95% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

white

Solubilité

DMSO: 100 mg/mL
ethanol: 5 mg/mL

Conditions d'expédition

wet ice

Température de stockage

−20°C

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)

Clé InChI

SXKBTDJJEQQEGE-UHFFFAOYSA-N

Description générale

A cell-permeable, selective, reversible, and non-competitive allosteric inhibitor of PTP1B (IC50 = 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively). Binds to a novel site away from the catalytic pocket and inhibits PTP1B activity by preventing closure of the WPD loop. Also available in InSolution format (Cat. No. 539749.

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
PTP1B403
Product does not compete with ATP.
Reversible: yes
Target IC50: 4 µM and 8 µM for PTP1B403 and PTP1B298, respectively

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Wiesmann, C., et al. 2004. Nat. Struct. Mol. Biol.11, 730.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Vitor Ferreira et al.
Redox biology, 63, 102741-102741 (2023-05-26)
Olanzapine (OLA), a widely used second-generation antipsychotic (SGA), causes weight gain and metabolic alterations when administered orally to patients. Recently, we demonstrated that, contrarily to the oral treatment which induces weight gain, OLA administered via intraperitoneal (i.p.) in male mice
Sarah Zierold et al.
Journal of the American Heart Association, 10(6), e018322-e018322 (2021-03-06)
Background Brain-derived neurotrophic factor (BDNF) is expressed in neuronal and nonneuronal cells and may affect vascular functions via its receptor, tropomyosin-related kinase B (TrkB). In this study, we determined the expression of BDNF in different perivascular adipose tissue (PVAT) depots
Bo Gong et al.
Nature, 631(8020), 415-423 (2024-06-13)
Directed cell migration is driven by the front-back polarization of intracellular signalling1-3. Receptor tyrosine kinases and other inputs activate local signals that trigger membrane protrusions at the front2,4-6. Equally important is a long-range inhibitory mechanism that suppresses signalling at the
Hyo Jeong Kim et al.
Frontiers in neuroscience, 15, 725398-725398 (2021-10-26)
Rett syndrome (RTT) is a severe X-linked dominant neurodevelopmental disorder caused by mutations in the methyl-CpG-binding protein 2 (MECP2) gene; MeCP2 regulates the expression of brain-derived neurotrophic factor (BDNF) and increasing BDNF levels ameliorates RTT symptoms. However, the clinical application

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