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.
동의어(들):
Lavendustin A, 5-Amino-[(N-2,5-dihydroxybenzyl)-Nʹ-2-hydroxybenzyl]salicylic Acid, RG14355
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모든 사진(1)
About This Item
추천 제품
Quality Level
분석
≥95% (HPLC)
형태
solid
제조업체/상표
Calbiochem®
저장 조건
OK to freeze
protect from light
색상
off-white
solubility
ethanol: 10 mg/mL
DMSO: soluble
배송 상태
ambient
저장 온도
−20°C
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 key
ULTTYPMRMMDONC-UHFFFAOYSA-N
일반 설명
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.
생화학적/생리학적 작용
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
경고
Toxicity: Standard Handling (A)
제조 메모
Further dilute with aqueous buffer just prior to use.
재구성
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
기타 정보
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.
법적 정보
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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.
Cellular oncogenes and retroviruses.
Annual review of biochemistry, 52, 301-354 (1983-01-01)
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
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
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