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530197 CD45 Inhibitor VI - CAS 130089-98-4 - Calbiochem

A cell-permeable, potent, irreversible, non-substrate competitive inhibitor of CD45/PTPRC tyrosine phosphatase activity (IC₅₀ = 290 nM).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 2-(4-Acetylanilino)-3-chloronaphthoquinone, Compound 211, Protein Tyrosine Phosphatase CD45 Inhibitor VI, PTP Inhibitor XXXII

Primary Target: CD45
530197
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
130089-98-4C₁₈H₁₂ClNO₃

Products

RéférenceConditionnement Qté
5301970001 Flacon en verre 10 mg
Description
OverviewA cell-permeable chloronaphthoquinone compound that potently inhibits CD45/PTPRC tyrosine phosphatase activity (IC50 = 290 nM) in a non-substrate-competitive and irreversible manner via targeting an allosteric pocket at the D1-D2 domains interface. Exhibits good selectivity over MKPX, PRL-2, PTP1B/PTPN1, TC-PTP/PTPN2, SHP-1/PTPN6, PEP/PTPN22, LAR/PTPRF, and PTP-Sigma/PTPRS (IC50 >40 µM). Shown to reduce T cell receptor-mediated activation of Lck, Zap-70, MAPK, and IL-2 production in primary T cells and effectively block human Lck pY-394 dephosphorylation in Jurkat, but not CD45-deficient J45.01 line, reducing cellular metabolic activity without affecting viability. Displays immunosuppressive properties against footpad swelling in a murine modle of delayed type hypersensitivity among C57/BL6 mice even when administered (3 mg/kg, i.p) after early onset of inflammation. However, it does not clear existing edema when applied to mice with fully developed inflammation.
Catalogue Number530197
Brand Family Calbiochem®
Synonyms2-(4-Acetylanilino)-3-chloronaphthoquinone, Compound 211, Protein Tyrosine Phosphatase CD45 Inhibitor VI, PTP Inhibitor XXXII
References
ReferencesPerron, M., et al. 2014. Mol. Pharmacol. 85, 553.
Product Information
CAS number130089-98-4
FormOrange powder
Hill FormulaC₁₈H₁₂ClNO₃
Chemical formulaC₁₈H₁₂ClNO₃
ReversibleN
Quality LevelMQ100
Applications
Biological Information
Primary TargetCD45
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
5301970001 04055977261301

Documentation

CD45 Inhibitor VI - CAS 130089-98-4 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

CD45 Inhibitor VI - CAS 130089-98-4 - Calbiochem Certificats d'analyse

TitreNuméro de lot
530197

Références bibliographiques

Aperçu de la référence bibliographique
Perron, M., et al. 2014. Mol. Pharmacol. 85, 553.
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision04-June-2014 JSW
Synonyms2-(4-Acetylanilino)-3-chloronaphthoquinone, Compound 211, Protein Tyrosine Phosphatase CD45 Inhibitor VI, PTP Inhibitor XXXII
DescriptionA cell-permeable chloronaphthoquinone that potently inhibits CD45/PTPRC tyrosine phosphatase activity (IC50 = 290 nM; substrate = 1 mM pp60-src pY-527 peptide) in a non-substrate-competitive, irreversible, and selective manner via targeting an allosteric pocket at the D1-D2 domains interface away from the substrate-binding/catalytic site, exhibiting little potency toward murine PEST or eight human phosphatases (IC50 > 40 µM against pNPP hydrolysis by MKPX, PRL-2, PTP1B/PTPN1, TC-PTP/PTPN2, SHP-1/PTPN6, PEP/PTPN22, LAR/PTPRF, and PTP-Sigma/PTPRS). Shown to increase human Lck pY394 phosphorylation level in Jurkat cells (by 40% in 24 h; 0.5 µM), but not CD45-deficient J45.01 line. Likewise, drug treatment effectively suppresses induction of Lck pY394, Zap-70 pY319, pErk1/2 phosphorylations and IL-2 release in primary murine splenocyte cultures upon T-cell activation (0.5 µM for 48 h) via TCR cross-linking with concomitant reduced metabolic activity (by MTT assay), but not cell death (by Trypan Blue exclusion). Single intraperitoneal injection (3 mg/kg) administered either 1 h or 3 d post Ovalbumin-/OVA-challenge (1 µg /footpad) among OVA-sensitized mice effectively prevents footpad swelling 6 d post challenge (<0.05 mm vs. >0.3 mm, respectively, with or without treatment) in delayed type hypersensitivity (DTH) tests in vivo. Exhibits no detectable cytotoxicity in KB or HEK293 cultures (0.5 µM for 24 h), while a 50% lymphocytes reduction is reported in mice 24 h post 3 mg/kg i.p. dosage with no other apparent adverse effects.
FormOrange powder
Intert gas (Yes/No) Packaged under inert gas
CAS number130089-98-4
Chemical formulaC₁₈H₁₂ClNO₃
Purity≥98% by HPLC
SolubilityDMSO (25 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesPerron, M., et al. 2014. Mol. Pharmacol. 85, 553.