428150
Lavendustin A
A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase and p60c-src with little effect on protein kinase A or protein kinase C.
同義詞:
Lavendustin A, 5-Amino-[(N-2,5-dihydroxybenzyl)-Nʹ-2-hydroxybenzyl]salicylic Acid, RG14355
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About This Item
暫時無法取得訂價和供貨情況
推薦產品
品質等級
化驗
≥95% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
off-white
溶解度
ethanol: 10 mg/mL
DMSO: soluble
運輸包裝
ambient
儲存溫度
−20°C
SMILES 字串
N(Cc3c(ccc(c3)O)O)(Cc2c(cccc2)O)c1cc(c(cc1)O)C(=O)O
InChI
1S/C21H19NO6/c23-16-6-8-19(25)14(9-16)12-22(11-13-3-1-2-4-18(13)24)15-5-7-20(26)17(10-15)21(27)28/h1-10,23-26H,11-12H2,(H,27,28)
InChI 密鑰
ULTTYPMRMMDONC-UHFFFAOYSA-N
一般說明
A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase (IC50 = 11 nM) and p60c-src (IC50 = 500 nM) with little effect on protein kinase A or protein kinase C (IC50 >200 µM). Also inhibits NMDA-stimulated cGMP production (IC50 = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor (VEGF) in rats.
A cell-permeable, reversible, substrate competitive, and potent inhibitor of EGF receptor tyrosine kinase (IC50 = 11 nM) and pp60c-src (IC50 = 500 nM) with little effect on protein kinase A or protein kinase C (IC50 >200 µM). Also inhibits NMDA-stimulated cGMP production (IC50 = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor in rats.
生化／生理作用
Cell permeable: yes
Primary Target
EGF receptor tyrosine kinase
EGF receptor tyrosine kinase
Product does not compete with ATP.
Reversible: yes
Target IC50: 11 nM and 500 nM against EGF receptor tyrosine kinase and p60c-src, respectively
警告
Toxicity: Standard Handling (A)
準備報告
Further dilute with aqueous buffer just prior to use.
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
其他說明
Hu, D.E., and Fan, T.-P. 1995. Br. J. Pharmacol. 114, 262.
Rodriguez, J., et al. 1994. Neuropharmacology 33, 1267.
Hsu, C.-Y., et al. 1991. J. Biol. Chem.266, 21105.
O’Dell, T.J., et al. 1991. Nature 353, 558; Onoda, T., et al. 1989. J. Nat. Prod.52, 1252.
Bishop, J.M. 1983. Annu. Rev. Biochem. 52, 307.
Rodriguez, J., et al. 1994. Neuropharmacology 33, 1267.
Hsu, C.-Y., et al. 1991. J. Biol. Chem.266, 21105.
O’Dell, T.J., et al. 1991. Nature 353, 558; Onoda, T., et al. 1989. J. Nat. Prod.52, 1252.
Bishop, J.M. 1983. Annu. Rev. Biochem. 52, 307.
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
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號，寫有 ‘Lot’或‘Batch’.。
J Rodriguez et al.
Neuropharmacology, 33(11), 1267-1274 (1994-11-01)
In striatal neurones in culture, N-methyl-D-aspartate-(NMDA), kainate-(Kai) and K(+)-dependent cGMP production is entirely mediated via nitric oxide (NO). Low concentrations of lavendustin-A (< or = 0.3 microM), a highly specific tyrosine kinase inhibitor, reduced irreversibly and in a time-dependent manner
T J O'Dell et al.
Nature, 353(6344), 558-560 (1991-10-10)
Long-term potentiation (LTP) in the hippocampus is thought to contribute to memory formation. In the Ca1 region, LTP requires the NMDA (N-methyl-D-aspartate) receptor-dependent influx of Ca2+ and activation of serine and threonine protein kinases. Because of the high amount of
Cellular oncogenes and retroviruses.
J M Bishop
Annual review of biochemistry, 52, 301-354 (1983-01-01)
D E Hu et al.
British journal of pharmacology, 114(2), 262-268 (1995-01-01)
1. Vascular endothelial growth factor (VEGF) is a heparin-binding angiogenic factor which specifically acts on endothelial cells via distinct membrane-spanning tyrosine kinase receptors. Here we used the rat sponge implant model to test the hypothesis that the angiogenic activity of
C Y Hsu et al.
The Journal of biological chemistry, 266(31), 21105-21112 (1991-11-05)
Lavendustin-A was reported to be a potent tyrosine kinase inhibitor of the epidermal growth factor (EGF) receptor (Onoda, T., Iinuma, H., Sasaki, Y., Hamada, M., Isshibi, K., Naganawa, H., Takeuchi, T., Tatsuta, K., and Umezawa, K. (1989) J. Nat. Prod.
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