Lenaldekar (LDK) 1PC X 10MG

Code: 5310680001 D2-231

Biochem/physiol Actions

Reversible: yes

Target IC50: 3 µM to block proliferation of T lymphocytes

Cell permeable: yes

General descri...


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€161.50 EACH
€198.65 inc. VAT

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)

assay≥98% (HPLC)
coloryellow
formpowder
manufacturer/tradenameCalbiochem®
Quality Level100
solubilityDMSO: 100 mg/mL
storage conditionprotect from light, OK to freeze
storage temp.2-8°C
Cas Number418800-15-4
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