| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cysteine cathepsins B, L, and S. GB111-NH2 is a potent and selective inhibitor of cysteine cathepsins, a family of lysosomal proteases involved in various physiological and pathological processes. Cathepsins B, L, and S are overexpressed in many cancers and play roles in tumor invasion, metastasis, and angiogenesis. By inhibiting these proteases, GB111-NH2 can modulate the tumor microenvironment. Its structural features allow for fluorescent tagging, making it useful for imaging and profiling applications.
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| ln Vitro |
In vitro, GB111-NH2 hydrochloride inhibits the enzymatic activity of cathepsins B, L, and S. Enzyme activity is measured using fluorogenic peptide substrates, and the IC50 values for inhibition are determined. It demonstrates selectivity for cysteine cathepsins over other protease classes. In cancer cell lines, treatment with GB111-NH2 can reduce invasive potential and modulate signaling pathways related to the tumor microenvironment. Its compatibility with fluorescent tags allows for visualization of cathepsin activity in live cells.
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| ln Vivo |
In vivo activity data for GB111-NH2 hydrochloride are limited to its use in imaging and mechanistic studies. The compound is used to study protease-driven tumor microenvironment remodeling in animal models. When conjugated to fluorescent probes, it can be used for in vivo imaging to visualize cathepsin activity in tumors. Its efficacy in modulating tumor progression in vivo has not been extensively reported. Specific in vivo studies are likely focused on its utility as a research tool rather than as a therapeutic agent.
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| Enzyme Assay |
In vitro enzyme assays for GB111-NH2 involve measuring the inhibition of cathepsin activity. Recombinant or purified cathepsins B, L, and S are incubated with a fluorogenic peptide substrate (e.g., Z-FR-AMC for cathepsin L) in the presence of varying concentrations of the inhibitor. The release of fluorescence is monitored over time, and the IC50 value is calculated. Selectivity is assessed by testing against other proteases, such as cathepsin K or matrix metalloproteinases. These cell-free assays confirm the compound's potency and selectivity.
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| Cell Assay |
In vitro cell-based assays for GB111-NH2 are performed in cancer cell lines. Cells are treated with the compound, and cathepsin activity is measured using cell-permeable fluorogenic substrates. Cell viability is assessed using standard assays such as MTT. The effect on cell invasion is evaluated using Boyden chamber assays. The compound can be conjugated to fluorescent tags for imaging intracellular cathepsin activity and localization. These assays are used to study the role of cathepsins in cancer cell biology.
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| Animal Protocol |
Specific in vivo animal experimental protocols for GB111-NH2 hydrochloride are not detailed in the available literature. As a research tool for imaging and protease profiling, it may be used in mouse models of cancer. Tumor-bearing mice are administered the compound (potentially as a fluorescent conjugate), and imaging is performed to visualize cathepsin activity. Tissues may be harvested for ex vivo analysis. These studies focus on understanding the role of cathepsins in the tumor microenvironment rather than evaluating therapeutic efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GB111-NH2 hydrochloride are not reported in the available literature. As a research tool, its PK profile is not the primary focus. The compound is typically used in vitro or for local administration in imaging studies. Its molecular weight is 610.14. Its solubility, half-life, and bioavailability are unknown. The hydrochloride salt form is used to enhance aqueous solubility. Standard PK studies would be required for drug development, but these are not available.
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| Toxicity/Toxicokinetics |
Toxicological data for GB111-NH2 hydrochloride are not detailed in the available literature. It is a research compound not intended for human use. No LD50 values or repeated-dose toxicity studies have been reported. Standard safety pharmacology studies have not been performed. As with all research chemicals, appropriate safety precautions should be taken when handling. Its specific toxicity profile has not been established.
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| References | |
| Additional Infomation |
GB111-NH2 hydrochloride is a potent and selective cysteine cathepsin inhibitor targeting cathepsins B, L, and S. Its molecular formula is C33H40ClN3O6, and its molecular weight is 610.14. It is used in cancer research and imaging studies due to its compatibility with fluorescent tagging. It supports mechanistic studies of protease-driven tumor microenvironment remodeling. It is available for research use only.
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| Molecular Formula |
C33H40CLN3O6
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| Molecular Weight |
610.14
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~125 mg/mL (~204.87 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (8.19 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6390 mL | 8.1948 mL | 16.3897 mL | |
| 5 mM | 0.3278 mL | 1.6390 mL | 3.2779 mL | |
| 10 mM | 0.1639 mL | 0.8195 mL | 1.6390 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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