5.31068

Lenaldekar (LDK)

• Synonyme(s) : Lenaldekar (LDK), T Cell Proliferation Inhibitor, LDK
• Formule empirique (notation de Hill): C₁₈H₁₄N₄
• Numéro CAS: 418800-15-4
• Poids moléculaire : 286.33
• Code UNSPSC : 51111800
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

A quinolinyl hydrazone derived compound that specifically blocks the proliferation of T cells in a dose-dependent manner (IC₅₀ = 3 µM in CD3+, CD4+, and CD8+ cells) without affecting other cell types. Its anti-proliferative effects are non-cytolytic in nature. Induces cell cycle delay at G2/M phase. Selectively induces apoptosis in human leukemic blasts and is shown to be active against all acute lymphoblastic leukemia cell lines (IC₅₀ = 1 -2 µM) and also displays in vivo activity in a zebrafish T-ALL model. Reduces the growth of human T-ALL in murine xenograft models (16 mg/kg, i,p, b.i.d). Also shown to specifically block myelin specific T cell responses and reduce inflammation and demyelination in experimental autoimmune encephalomyelitis, possibly via its interactions with insulin-like growth factor-1 receptor. Diminishes the phosphorylation of T308 and S473 on Akt, however, its action is believed to be upstream of PI-3K/Akt. Does not affect the activity of over 450 other kinases in any significant manner. Exhibits a plasma t1/2 = 2 h.

A quinolinyl hydrazone derived compound that specifically blocks the proliferation of T cells in a dose-dependent manner (IC₅₀ = 3 µM in CD3+, CD4+, and CD8+ cells) without affecting other cell types. Its anti-proliferative effects are non-cytolytic in nature. Induces cell cycle delay at G2/M phase. Selectively induces apoptosis in human leukemic blasts and is shown to be active against all acute lymphoblastic leukemia cell lines (IC₅₀ = 1 -2 µM) and also displays in vivo activity in a zebrafish T-ALL model. Reduces the growth of human T-ALL in murine xenograft models (16 mg/kg, i,p, b.i.d). Also shown to specifically block myelin specific T cell responses and reduce inflammation and demyelination in experimental autoimmune encephalomyelitis, possibly via its interactions with insulin-like growth factor-1 receptor. Diminishes the phosphorylation of T308 and S473 on Akt, however, its action is believed to be upstream of PI-3K/Akt. Does not affect the activity of over 450 other kinases in any significant manner. Exhibits a plasma t1/2 = 2 h.

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

Actions biochimiques/physiologiques

Cell permeable: yes

Reversible: yes

Target IC₅₀: 3 µM to block proliferation of T lymphocytes

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 3 months at -20°C.

Autres remarques

Cusick, M.F., et al. 1999. PNAS.96, 12192.
Ridges, S, et al. 2012. Blood.119, 5621.

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