5.30654

c-Rel Inhibitor, IT-603

• Synonyme(s) : c-Rel Inhibitor, IT-603, (5 Z)-5-((5-Bromo-2-hydroxy-3-methoxyphenyl)methylidene)-2-sulfanylideneimidazolidin-4-one, (5 Z)-5-(5-Bromo-2-hydroxy-3-methoxybenzylidene)-2-thioxo-4-imidazolidinone, IT603, (5Z)-5-((5-Bromo-2-hydroxy-3-methoxyphenyl)methylidene)-2-sulfanylideneimidazolidin-4-one, (5Z)-5-(5-Bromo-2-hydroxy-3-methoxybenzylidene)-2-thioxo-4-imidazolidinone, IT603
• Formule empirique (notation de Hill): C₁₁H₉BrN₂O₃S
• Numéro CAS: 292168-90-2
• Poids moléculaire : 329.17
• Code UNSPSC : 51111800
• ID de substance PubChem : 840180
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: dark yellow
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: COC1=CC(=CC(=C1O)C=C2C(=O)NC(=S)N2)Br

Description

Description générale

A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC₅₀ = 3 µM in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC₅₀ = 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).

A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC₅₀ = 3 µM in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC₅₀ = 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
c-Rel

Reversible: yes

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.

Use only fresh DMSO for reconstitution.

Autres remarques

Shono, Y., et al. 2014. Cancer Discovery4, 578.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable