| Size | Price | Stock | Qty |
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| 1mg |
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| 500mg | |||
| Other Sizes |
| Targets |
IC50: <0.5 mM[1]
TG-2-IN-4 targets transglutaminase 2 (TG2), a calcium-dependent enzyme that catalyzes the cross-linking of proteins by forming isopeptide bonds between glutamine and lysine residues. TG2 is a multifunctional protein that also possesses GTPase activity and is involved in various cellular processes including apoptosis, cell adhesion, wound healing, and extracellular matrix remodeling. In inflammatory diseases, TG2 has been implicated in the pathogenesis of conditions such as celiac disease, fibrosis, and inflammatory bowel disease. By inhibiting TG2, TG-2-IN-4 may modulate these processes. |
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| ln Vitro |
TG-2-IN-4 shows in vitro inhibition of transglutaminase 2 with an IC50 of less than 0.5 mM. This activity has been validated in biochemical assays measuring TG2-mediated cross-linking activity. The compound's ability to inhibit TG2 makes it a useful tool for studying the role of this enzyme in various biological and pathological contexts. The specific IC50 value (<0.5 mM) indicates moderate potency, which may be sufficient for research applications.
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| ln Vivo |
In vivo activity of TG-2-IN-4 has been suggested for research applications in inflammatory diseases. By inhibiting TG2, the compound may modulate inflammatory responses and tissue remodeling processes. However, detailed in vivo efficacy data have not been extensively reported in the available literature. The compound is primarily used as a research tool for in vitro and ex vivo studies.
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| Enzyme Assay |
Non-cell-based enzyme assays for TG-2-IN-4 typically involve measuring the inhibition of recombinant TG2 activity using a fluorogenic substrate. A standard protocol includes: incubating purified TG2 enzyme with a substrate such as monodansylcadaverine (MDC) and N,N-dimethylcasein in assay buffer (pH 7.5) containing 5 mM CaCl2 and 2 mM DTT. TG-2-IN-4 is added at various concentrations (typically 0.001–1000 μM), and the incorporation of MDC into casein is monitored by fluorescence at excitation/emission wavelengths of 335/500 nm. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for TG-2-IN-4 typically involve cell lines expressing TG2 or relevant to inflammatory diseases. A representative protocol includes: culturing cells (e.g., macrophages or epithelial cells) in appropriate medium, treating with TG-2-IN-4 at various concentrations (0.1–1000 μM) for 24–72 hours, and measuring TG2 activity in cell lysates using a fluorogenic substrate. TG2 expression and activity can be modulated by inflammatory stimuli such as TNFα or IL-1β. Cell viability is assessed to ensure that observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo animal studies with TG-2-IN-4 have not been extensively reported in the available literature. If conducted, a typical protocol would involve mouse models of inflammatory diseases such as DSS-induced colitis, carrageenan-induced paw edema, or bleomycin-induced fibrosis. Administration of TG-2-IN-4 via oral gavage or intraperitoneal injection would be followed by assessment of inflammatory markers, histopathological analysis of target tissues, and evaluation of clinical disease scores.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TG-2-IN-4 have not been extensively reported in the available literature. As a small molecule with a molecular weight of 612.72 g/mol, it is expected to have moderate oral bioavailability and tissue distribution. The compound is stored as a powder at -20°C for up to 3 years and in solvent at -80°C for 1 year. Solubility information is available for formulation in DMSO and other solvents.
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| Toxicity/Toxicokinetics |
As a research compound, TG-2-IN-4 is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity. The compound is stored as a powder at -20°C for up to 3 years.
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| References | |
| Additional Infomation |
TG-2-IN-4 (Compound 8, CAS 2410899-01-1) is a transglutaminase 2 inhibitor with an IC50 of less than 0.5 mM. The compound is utilized in the study of inflammatory disorders, where TG2 plays a pathogenic role. TG2 is a validated target in celiac disease, fibrosis, and inflammatory bowel disease, and TG-2-IN-4 provides researchers with a tool to investigate the therapeutic potential of TG2 inhibition. The compound is available in high purity (99.62%) and is suitable for both in vitro and in vivo studies.
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| CAS # |
2410899-01-1
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|---|---|
| Appearance |
Off-white to yellow 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 |
| 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) |
Typically soluble in DMSO (e.g. 10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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