| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
TJ191 specifically targets malignant T-cells characterized by low expression of the transforming growth factor β type III receptor (TβRIII). Its sensitivity is inversely correlated with TβRIII expression, making this receptor a predictive biomarker for the compound's activity. TJ191 selectively inhibits the function of TβRIII, which provides a crucial target for cancer research. The compound's mechanism of action is highly selective, as it does not affect the proliferation of other cancer cells, normal fibroblasts, or immune cells.
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| ln Vitro |
TJ191 (0-100 µM; 24 hours) significantly inhibits the growth of malignant cell lines; its IC50 values in CEM, JURKAT, MOLT-3, MOLT-4, MT-2, C8166, and HSB-2 cells are 0.13 µM, 0.13±0.08 µM, 0.26±0.19 µM, 0.22±0.11 µM, 1.5±0.02 µM, 0.32 ±0.086 µM, 3.1±0.5 µM, and 0.26±0.16 µM, respectively. However, HUT-78 (IC50=17±10 µM) and MT-4 (IC50=47 ± 5 µM) cells are unaffected [1]. TJ191 (0.1-3 µM; 8 or 24 hours) causes CEM cells to undergo apoptosis in a way that is dependent on both concentration and time. After 24 hours, TJ191 promotes up to 80% cell death even at a dosage of 0.3 µM [1].
In vitro, TJ191 exhibits pronounced and specific anti-proliferative activity against various T-cell malignant cell lines. Its IC50 values are exceptionally low in sensitive lines such as CEM (0.13 µM), JURKAT (0.13 µM), and MOLT-3 (0.26 µM). In CEM cells, TJ191 (0.1-3 µM; 8 or 24 hours) induces apoptosis in a concentration- and time-dependent manner. Remarkably, even at a low concentration of 0.3 µM, it induces a maximum apoptotic rate of 80% after 24 hours. In contrast, it shows no significant effect on cells like HUT-78 (IC50=17 µM) and MT-4 (IC50=47 µM), underscoring its selectivity. |
| ln Vivo |
In vivo studies have demonstrated that TJ191 inhibits the growth of prostate cancer cells. It selectively targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells, which can be studied in appropriate xenograft models. The compound's high selectivity suggests it would be effective in vivo against tumors with low TβRIII expression while sparing normal tissues. Its utility in cancer research is supported by its potent and specific activity against malignant T-cells.
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| Enzyme Assay |
Cell-free assays for TJ191 are not standard because its activity is defined by its selective cellular effects. However, its target engagement can be studied using binding assays with TβRIII or related proteins. Its purity (>99%) and molecular properties can be confirmed by standard analytical techniques like HPLC and mass spectrometry. Assays can also measure its ability to inhibit the activation of the growth factor-β1 receptor.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Malignant T-cell Leukemia/Lymphoma Cell Tested Concentrations: 0.01 µM, 0.1 µM, 1 µM, 10 µM, 100 µM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated inhibitory effect on drug-sensitive cells, IC50 Range is 0.13 µM to 3.1 µM. Apoptosis analysis[1] Cell Types: CEM Cell Line Tested Concentrations: 0.1-3 µM Incubation Duration: 8 or 24 hrs (hours) Experimental Results: Caused apoptosis. Cellular assays for TJ191 evaluate its anti-proliferative and pro-apoptotic effects. Cells are treated with TJ191 (0-100 µM; 24 hours), and cell viability is measured using standard assays like MTT or CellTiter-Glo to determine IC50 values. Apoptosis is assessed by flow cytometry using annexin V/PI staining. Its selectivity is confirmed by testing its effects on a panel of malignant and normal cell lines. TJ191 has no effect on normal fibroblasts or immune cells. |
| Animal Protocol |
In vivo animal experiments for TJ191 are conducted in xenograft models of T-cell leukemia/lymphoma or prostate cancer. Immunocompromised mice are implanted with human cancer cells and treated with TJ191, typically via oral or intraperitoneal administration. Tumor growth inhibition, survival, and pharmacodynamic markers are assessed. The compound's selectivity ensures that it targets tumors with low TβRIII expression while minimizing off-target effects.
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| ADME/Pharmacokinetics |
TJ191 has a molecular weight of 255.38 g/mol and a molecular formula of C13H21NO2S. It is a solid powder soluble in DMSO (up to 100 mg/mL) but insoluble in water. For in vivo use, it can be formulated as a suspension in CMC-Na (up to 5 mg/mL) or in a solution of 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline. The powder is stable for up to 3 years at -20°C. Its SMILES notation is CCCCCCCC1=CC(=C(S1)N)C(=O)OC.
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| Toxicity/Toxicokinetics |
The toxicological profile of TJ191 is favorable due to its high selectivity. It has no effects on the proliferation of normal fibroblasts or immune cells, suggesting a wide therapeutic window. Standard toxicology studies would be necessary to fully assess its safety, but its selectivity reduces the risk of off-target toxicities commonly associated with classical chemotherapeutics.
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| References | |
| Additional Infomation |
TJ191 is a potent and selective anti-cancer research compound that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells. Its selectivity is validated by CRISPR technology and is inversely correlated with TβRIII expression. It has been used to study T-cell malignancies and prostate cancer. TJ191 is not an approved drug and is for research use only. It is also known as TJ-191 or TJ 191.
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| Molecular Formula |
C13H21NO2S
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| Molecular Weight |
255.376342535019
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| Exact Mass |
255.129
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| CAS # |
1522415-97-9
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| PubChem CID |
72704992
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
17
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| Complexity |
236
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=C(C(=O)OC)C=C1CCCCCCC)N
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| InChi Key |
HUFNXSPJUAHQHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H21NO2S/c1-3-4-5-6-7-8-10-9-11(12(14)17-10)13(15)16-2/h9H,3-8,14H2,1-2H3
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| Chemical Name |
methyl 2-amino-5-heptylthiophene-3-carboxylate
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| Synonyms |
TJ 191; TJ-191; TJ191
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~391.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.79 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (9.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9157 mL | 19.5787 mL | 39.1573 mL | |
| 5 mM | 0.7831 mL | 3.9157 mL | 7.8315 mL | |
| 10 mM | 0.3916 mL | 1.9579 mL | 3.9157 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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