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p-Aminophenylmercuric acetate

(Synonyms: APMA) 目录号 : GC69651 复制 一键复制产品信息

p-Aminophenylmercuric acetate是一种有机汞化合物,可作为MMP激活剂,能够作用于蛋白质巯基或诱导与MMP-8激活和抑制均相关的半胱氨酸转换反应。

p-Aminophenylmercuric acetate Chemical Structure

Cas No.:6283-24-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥545.00
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50mg
¥495.00
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100mg
¥810.00
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Description

p-Aminophenylmercuric acetate, an organomercurial MMP activator capable of attacking protein sulfhydryl groups or inducing cysteine switch reactions involved in both the activation and inhibition of MMP-8 [1]. p-Aminophenylmercuric acetate can convert the latent form of MMP-9 (94kDa) purified from the human cell line HL-60 into an intermediary active form (84kDa)[2]. p-Aminophenylmercuric acetate can be used as a building block to synthesize novel types of photochromic dyes[3].

In vitro, p-Aminophenylmercuric acetate (30µM; 20min) reduced the number of dihydromorphane binding sites in rat brain homogenate and increased the sensitivity of the agonist to the inhibitory effect on sodium binding[4]. p-Aminophenylmercuric acetate treatment (100µM) for 1h activated the betacellulin precursor (pro-BTC) shedding in Wild-type dermal fibroblasts transfected with BTC-hemagglutinin (HA)[5]. Treatment with p-Aminophenylmercuric acetate (>0.3μg/ml) for 24 hours significantly induced the death of murine lymphocytes[6].

References:
[1] Gendron R, Grenier D, Sorsa T, et al. Inhibition of the activities of matrix metalloproteinases 2, 8, and 9 by chlorhexidine[J]. Clinical Diagnostic Laboratory Immunology, 1999, 6(3): 437-439.
[2] Backstrom J R, Tökés Z A. The 84‐kDa form of human matrix metalloproteinase‐9 degrades substance P and gelatin[J]. Journal of neurochemistry, 1995, 64(3): 1312-1318.
[3] Kanakkanatt S V, Patel V S, Patel R G, et al. Novel Methods of Synthesis of Dithizonate Type Photochromic Dyes & Polymers[J]. Molecular Crystals and Liquid Crystals Science and Technology. Section A. Molecular Crystals and Liquid Crystals, 1994, 246(1): 159-168.
[4] PASTERNAK G W, WILSON H A, SNYDER S H. Differential effects of protein-modifying reagents on receptor binding of opiate agonists and antagonists[J]. Molecular Pharmacology, 1975, 11(3): 340-351.
[5] Sanderson M P, Erickson S N, Gough P J, et al. ADAM10 mediates ectodomain shedding of the betacellulin precursor activated by p-aminophenylmercuric acetate and extracellular calcium influx[J]. Journal of Biological Chemistry, 2005, 280(3): 1826-1837.
[6] Kim H M, Hong D H, Lee C W, et al. Studies on cell-specific cytotoxicities induced by p-aminophenyl-mercuric acetate (APMA)[J]. The Journal of Toxicological Sciences, 1998, 23(SupplementIV): 653-656.

p-Aminophenylmercuric acetate是一种有机汞化合物,可作为MMP激活剂,能够作用于蛋白质巯基或诱导与MMP-8激活和抑制均相关的半胱氨酸转换反应[1]。p-Aminophenylmercuric acetate能将从人源细胞系HL-60中纯化的无活性前体形式MMP-9(94kDa)转化为中间活性形式(84kDa)[2]。p-Aminophenylmercuric acetate可作为结构单元用于合成新型光致变色染料[3]

在体外,p-Aminophenylmercuric acetate处理(30µM;20分钟)减少了大鼠脑匀浆中二氢吗啡结合位点的数量,并提高了激动剂对钠结合抑制效应的敏感性[4]。p-Aminophenylmercuric acetate处理(100µM)1小时激活了转染BTC-hemagglutinin (HA)的野生型皮肤成纤维细胞中betacellulin前体(pro-BTC)的脱落过程[5]。使用浓度高于0.3µg/ml的p-Aminophenylmercuric acetate处理24小时,可显著诱导小鼠淋巴细胞死亡[6]

实验参考方法

Cell experiment [1]:

Cell lines

Wild-type dermal fibroblasts transfected with BTC-HA

Preparation Method

Wild-type dermal fibroblasts transfected with BTC-HA were seeded at a density of 1×105 cells per well in a 6-well plate. Cells were cultured in a medium containing IFN-γ at 33°C for 48 hours until confluence was reached, and then further cultured in a medium without IFN-γ at 37°C for 36 hours. To evaluate the stimulation-induced pro-BTC shedding, the cells were cultured in serum-free DMEM medium containing or without p-Aminophenylmercuric acetate (100μM) for 1h. 30 minutes before the addition of the p-Aminophenylmercuric acetate, the cells were pre-incubated with GM6001, kinase inhibitors, or calcium-free DMEM. Then, the cell lysates were collected for analysis.

Reaction Conditions

100µM; 1h

Applications

p-Aminophenylmercuric acetate treatment activated the Pro-BTC shedding in wild-type dermal fibroblasts transfected with BTC-HA.

References:
[1] Sanderson M P, Erickson S N, Gough P J, et al. ADAM10 mediates ectodomain shedding of the betacellulin precursor activated by p-aminophenylmercuric acetate and extracellular calcium influx[J]. Journal of Biological Chemistry, 2005, 280(3): 1826-1837.

化学性质

Cas No. 6283-24-5 SDF Download SDF
别名 APMA
分子式 C8H9HgNO2 分子量 351.75
溶解度 DMSO : 125 mg/mL (355.37 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C
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1 mM 2.8429 mL 14.2146 mL 28.4293 mL
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10 mM 284.3 μL 1.4215 mL 2.8429 mL
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