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Merck
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文件

5.31068

Sigma-Aldrich

Lenaldekar (LDK)

别名:

Lenaldekar (LDK), T Cell Proliferation Inhibitor, LDK

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About This Item

经验公式(希尔记法):
C18H14N4
分子量:
286.33
分類程式碼代碼:
51111800
NACRES:
NA.77

化驗

≥98% (HPLC)

品質等級

形狀

powder

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

yellow

溶解度

DMSO: 100 mg/mL

儲存溫度

2-8°C

一般說明

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.

生化/生理作用

Cell permeable: yes
Reversible: yes
Target IC50: 3 µM to block proliferation of T lymphocytes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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