Glyoxalase I inhibitor
(Synonyms: L-GAMMA-谷氨酰基-S-[[(4-溴苯基)羟基氨基]羰基]-L-半胱氨酰甘氨酸二乙酯单盐酸盐) 目录号 : GC13038
Glyoxalase I inhibitor 是一种有效的 Glyoxalase I 抑制剂，是抗癌剂的候选药物。
Cas No.:221174-33-0
Sample solution is provided at 25 µL, 10mM.
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S-(N-Aryl-N-hydroxycarbamoyl)glutathione derivatives have been proposed as possible anticancer agents, because of their ability to strongly inhibit the methylglyoxal-detoxifying enzyme glyoxalase I. Glyoxalase I inhibitor is a potent inhibitor of glyoxalase I.
In vitro: As a tumor-selective anticancer agent, Glyoxalase I inhibitor [3(Et)2] was evaluated against B16 melanotic melanoma, L1210 murine leukemia, and nonproliferating murine splenic lymphocytes in culture. The diethyl ester prodrugs of Glyoxalase I inhibitor [3(Et)2] also displayed significant tumour-selective toxicity towards L1210 cells compared with normal murine splenic lymphocytes in vitro [1].
In vivo: Small-scale efficacy studies indicated that 3b(Et)2 could effectively inhibit tumour growth in plasma esterase-deficient mice bearing murine B16 melanoma and in esterasedeficient athymic nude mice bearing androgen-independent human prostate PC-3 tumours or human colon HT-29 tumours [2].
Clinical trial: No clinical data are available.
References:
[1] Kavarana MJ, Kovaleva EG, Creighton DJ, Wollman MB, Eiseman JL. Mechanism-based competitive inhibitors of glyoxalase I: intracellular delivery, in vitro antitumor activities, and stabilities in human serum and mouse serum. J Med Chem. 1999;42(2):221-8.
[2] Creighton DJ, Zheng ZB, Holewinski R, Hamilton DS, Eiseman JL. Glyoxalase I inhibitors in cancer chemotherapy. Biochem Soc Trans. 2003;31(Pt 6):1378-82.
| Cas No. | 221174-33-0 | SDF | |
| 别名 | L-GAMMA-谷氨酰基-S-[[(4-溴苯基)羟基氨基]羰基]-L-半胱氨酰甘氨酸二乙酯单盐酸盐 | ||
| 化学名 | ethyl (2S)-2-amino-5-[[(2R)-3-[(4-bromophenyl)-hydroxycarbamoyl]sulfanyl-1-[(2-ethoxy-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate hydrochloride | ||
| Canonical SMILES | CCOC(=O)CNC(=O)C(CSC(=O)N(C1=CC=C(C=C1)Br)O)NC(=O)CCC(C(=O)OCC)N.Cl | ||
| 分子式 | C21H30BrClN4O8S | 分子量 | 613.91 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light, stored under nitrogen |
| 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 | 1.6289 mL | 8.1445 mL | 16.289 mL |
| 5 mM | 0.3258 mL | 1.6289 mL | 3.2578 mL |
| 10 mM | 0.1629 mL | 0.8145 mL | 1.6289 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
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet