| Size | Price | Stock | Qty |
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| 250mg |
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| Targets |
Cystamine targets transglutaminase and caspase-3. It acts as an inhibitor of transglutaminase, an enzyme involved in protein crosslinking, and caspase-3, a key effector caspase in apoptosis. By inhibiting these enzymes, it modulates various cellular processes. It is used in Huntington's disease research.
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| ln Vitro |
Caspases-3 is inhibited by cystamine, with an IC50 value of 23.6 μM[1]. Recombinant active caspase-3 is inhibited by cystamine (0-500 μM; 0-16 hours) in a concentration-dependent manner [1]. Glutathione levels are markedly elevated by cystamine (250 μM; 10 hours) [1].
Cystamine inhibits transglutaminase and caspase-3 with an IC50 of 23.6 μM. It interferes with sulfhydryl enzymes. It has been shown to have protective effects against radiation and liver damage. It is used as a crosslinking agent in polymer chemistry. |
| ln Vivo |
R6/2 transgenic HD mice that receive cystamine (oral, i.p.; 112, 225 mg/kg) have reduced behavioral and neuropathological severity, decreased Tgase activity, and extended longevity [2].
Cystamine is an orally active transglutaminase inhibitor. It has been studied for its potential in treating Huntington's disease. It may protect against carbon tetrachloride liver damage. It is a radiation-protective agent. |
| Enzyme Assay |
Cystamine is evaluated in cell-free enzymatic assays using purified transglutaminase and caspase-3. The compound is incubated with the enzyme and a substrate, and the inhibition of enzyme activity is measured. IC50 values are determined to quantify the potency of inhibition.
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Human Neuroblastoma SH-SY5Y Cell Tested Concentrations: 250, 500 μM Incubation Duration: 0-16 h Experimental Results: Inhibition of MG132-mediated caspase-3 activation. Inhibits H2O2-mediated caspase-3 activation. Inhibits caspase-3 activity in a tTG-independent manner. Cystamine is assessed in cell-based assays to study its effects on transglutaminase and caspase-3 activity. Cells are treated with Cystamine, and enzyme activity is measured. Its effects on apoptosis and protein crosslinking are evaluated. |
| Animal Protocol |
Animal/Disease Models: R6/2 transgenic HD mice [2]
Doses: 112, 225 mg/kg Route of Administration: intraperitonealor po (po (oral gavage)) daily Experimental Results: Dramatically prolonged survival, improved body weight and exercise capacity, and delayed neuropathological sequelae And Dramatically altered neuropathological sequelae were the levels of Tgase activity and N(Sigma)-(gamma-L-glutamyl)-L-lysine (GGEL) levels. Cystamine is administered orally in animal models to evaluate its effects on Huntington's disease and liver damage. It has been shown to have protective effects. However, specific animal study protocols are not extensively documented. |
| ADME/Pharmacokinetics |
Cystamine has a molecular weight of 152.28 and a molecular formula of C4H12N2S2. It has a CAS number of 51-85-4. The compound is freely soluble in water and soluble in alcohol. It is a viscous oil that cannot be distilled without decomposition.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Cystamine. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized in the available literature.
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| References |
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| Additional Infomation |
Cystamine is an organic disulfide obtained by the oxidative dimerization of cysteamine. It is an EC 2.3.2.13 (protein-glutamine-γ-glutamyltransferase) inhibitor. It is an organic disulfide and primary amino compound functionally related to cysteamine. It is a radiation protectant that interferes with sulfhydryl enzymes. It may also have a protective effect against carbon tetrachloride-induced liver damage.
Cystamine is an orally active transglutaminase inhibitor. It has a CAS number of 51-85-4. It is used in research to study Huntington's disease, apoptosis, and protein crosslinking. It is also a radiation-protective agent. It is not approved for clinical use. |
| Molecular Formula |
C4H12N2S2
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| Molecular Weight |
152.27
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| Exact Mass |
152.044
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| CAS # |
51-85-4
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| Related CAS # |
Cystamine (dihydrochloride）;56-17-7
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| PubChem CID |
2915
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| Appearance |
Light yellow to brown liquid
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| Density |
1.172g/cm3
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| Boiling Point |
264.8ºC at 760 mmHg
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| Flash Point |
114ºC
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| Index of Refraction |
1.587
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| LogP |
1.685
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
8
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| Complexity |
37
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(CSSCCN)N
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| InChi Key |
APQPRKLAWCIJEK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C4H12N2S2/c5-1-3-7-8-4-2-6/h1-6H2
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| Chemical Name |
2-(2-aminoethyldisulfanyl)ethanamine
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| Synonyms |
Mercamine disulfide; Aminoethyl-SS-ethylamine; Cystamine
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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 |
| 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 : ~100 mg/mL (~656.69 mM)
H2O : ~100 mg/mL (~656.69 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (16.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (16.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (16.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.5673 mL | 32.8364 mL | 65.6728 mL | |
| 5 mM | 1.3135 mL | 6.5673 mL | 13.1346 mL | |
| 10 mM | 0.6567 mL | 3.2836 mL | 6.5673 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02304666 | Unknown | Procedure: Colonoscopy for biopsies samples |
Inflammatory Bowel Disease | Assistance Publique Hopitaux De Marseille |
November 2014 | Not Applicable |
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