Biochem/physiol Actions
Reversible: yes
Target IC50: 3 µM to block proliferation of T lymphocytes
Cell permeable: yes
General description
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Cusick, M.F., et al. 1999. PNAS.96, 12192.Ridges, S, et al. 2012. Blood.119, 5621.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria to qualify for the following awards: