Antipain (hydrochloride)
(Synonyms: 抗痛素二盐酸盐) 目录号 : GC40032Antipain (hydrochloride)是一种可逆性蛋白酶抑制剂。
Cas No.:37682-72-7
Sample solution is provided at 25 µL, 10mM.
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Antipain (hydrochloride) is a reversible protease inhibitor [1]. Antipain forms a hemiacetal adduct with the active serine in the active site of protease through its terminal aldehyde group, thereby inhibiting the activity of various proteases including serine proteases and cysteine proteases [2-3]. Antipain is commonly used in the study of tumors [4].
In hamster embryo cells, Antipain (6μg/mL; 24h) affects the fixation and expression of X-ray-induced neoplastic transformation by regulating DNA repair processes [5]. In BALB/c 3T3 cells, Antipain (10μM; 48h) treatment reduces the cell transformation rate induced by 3-MCA and 1,2-DBE [6].
References:
[1]. Suda H, AOYAGI T, HAMADA M, et al. Antipain, a new protease inhibitor isolated from agtinomycetes[J]. The Journal of antibiotics, 1972, 25(4): 263-265.
[2]. Otto H H, Schirmeister T. Cysteine proteases and their inhibitors[J]. Chemical reviews, 1997, 97(1): 133-172.
[3]. Nguyen Q V, Knapp W, Humphreys R E. Inhibition by leupeptin and antipain of the intracellular proteolysis of Ii[J]. Human immunology, 1989, 24(3): 153-163.
[4]. Nomura T, Enomoto T, Shibata K, et al. Antiteratogenic effects of tumor inhibitors, caffeine, antipain, and retinoic acid in mice[J]. Cancer research, 1983, 43(11): 5156-5162.
[5]. Borek C, Miller R, Pain C, et al. Conditions for inhibiting and enhancing effects of the protease inhibitor antipain on x-ray-induced neoplastic transformation in hamster and mouse cells[J]. Proceedings of the National Academy of Sciences, 1979, 76(4): 1800-1803.
[6]. Vaccari M, Argnani A, Horn W, et al. Effects of the protease inhibitor antipain on cell malignant transformation[J]. Anticancer research, 1999, 19(1A): 589-596.
Antipain (hydrochloride)是一种可逆性蛋白酶抑制剂 [1]。Antipain通过其末端醛基与蛋白酶活性位点的活性丝氨酸形成半缩醛加合物，从而抑制包括丝氨酸蛋白酶和半胱氨酸蛋白酶在内的多种蛋白酶的活性 [2-3]。Antipain常用于肿瘤研究 [4]。
在仓鼠胚胎细胞中，Antipain（6μg/mL；24h）通过调节DNA修复过程影响X射线诱导的肿瘤转化的固定和表达 [5]。在BALB/c 3T3细胞中，Antipain（10μM；48h）处理可降低3-MCA和1,2-DBE诱导的细胞转化率 [6]。
| Cell experiment [1]: | |
Cell lines | Hamster embryo cells |
Preparation Method | Cells were irradiated at room temperature,24h after plating, with 300rad of X-rays at a dose rate of 32.2rad/min and incubated at 37℃ with 5% CO2 in air, with weekly medium changes. The source of x-rays was a Siemens300kVp constant potential generator with an added filter of 0.2mm of copper. Controls consisting of unirradiated cultures with or without added Antipain were maintained under the same conditions as the experimental cultures. |
Reaction Conditions | 6μg/mL; 24h |
Applications | Antipain affects the fixation and expression of X-ray-induced neoplastic transformation by regulating DNA repair processes. |
References: | |
| Cas No. | 37682-72-7 | SDF | |
| 别名 | 抗痛素二盐酸盐 | ||
| 化学名 | N2-[[[(1S)-1-carboxy-2-phenylethyl]amino]carbonyl]-L-arginyl-N-[4-[(aminoiminomethyl)amino]-1-formylbutyl]-L-valinamide, dihydrochloride | ||
| Canonical SMILES | O=C(O)C(NC(N[C@@H](CCCNC(N)=N)C(N[C@@H](C(C)C)C(NC(C=O)CCCNC(N)=N)=O)=O)=O)CC1=CC=CC=C1.Cl.Cl | ||
| 分子式 | C27H44N10O6 • 2HCl | 分子量 | 677.6 |
| 溶解度 | H2O : 50 mg/mL (73.79 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4758 mL | 7.379 mL | 14.758 mL |
| 5 mM | 0.2952 mL | 1.4758 mL | 2.9516 mL |
| 10 mM | 0.1476 mL | 0.7379 mL | 1.4758 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet