Lenaldekar (LDK)

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.

Cell permeable: yes

Reversible: yes

Target IC₅₀: 3 µM to block proliferation of T lymphocytes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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

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