Glyoxalase I inhibitor |
| Catalog No.GC13038 |
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C21H30BrClN4O8S | M.Wt | 613.91 |
| Solubility | Soluble in DMSO | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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