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Merck
모든 사진(1)

문서

428150

Sigma-Aldrich

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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About This Item

실험식(Hill 표기법):
C21H19NO6
CAS Number:
Molecular Weight:
381.38
UNSPSC 코드:
12352200
NACRES:
NA.77

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
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.

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.

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문서 라이브러리 방문

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
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.
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
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

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