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| Targets |
Telomerase-IN-1 targets telomerase, the enzyme responsible for maintaining telomere length in eukaryotic cells. Telomerase is a ribonucleoprotein complex composed of a catalytic subunit (hTERT) and an RNA template (hTR). By inhibiting telomerase, the compound prevents the addition of telomeric repeats to chromosome ends, leading to progressive telomere shortening and ultimately cell senescence or apoptosis. Telomerase is activated in approximately 85-90% of human cancers, making it an attractive target for cancer therapy.
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| ln Vitro |
Our in vitro tests reveal that the title chemical (Telomerase-IN-1) has high inhibitory action against telomerase, high anti-proliferation ability on SMMC-7721 cells, and no clear harmful effects on normal human liver cells. Telomerase-IN-1 therapy inhibited cancer cell proliferation in a dose- and time-dependent manner; however, the viability of L-02 showed minimal modifications at 10 μM. Treatment of SMMC-7721 cells with telomerase-IN-1 (20, 40, and 80 nM) for 48 hours resulted in enhanced apoptosis. Treatment of SMMC-7721 cells with telomerase-IN-1 (20, 40, and 80 nM) for 48 hours resulted in a considerable accumulation of green fluorescence, indicating a reduction in MMPs. At 40 nM, telomerase-IN-1 dramatically boosts the expression of cyt-c and Bax, but reduces Bcl-2 levels [1].
In vitro studies have demonstrated that Telomerase-IN-1 is a potent inhibitor of telomerase activity, with an IC50 value in the low micromolar range. The compound inhibits telomerase activity in various cancer cell lines, leading to telomere shortening, cell cycle arrest, and apoptosis. The compound's selectivity for telomerase over other enzymes has been characterized. These in vitro activities support the compound's potential as an anticancer agent. |
| ln Vivo |
Our in vivo research demonstrates that telomerase-IN-1 considerably suppresses the growth of tumors in xenograft models. The findings demonstrate how endoplasmic reticulum stress (ERS) triggers the expression of hTERT via endoplasmic reticulum excessive response (EOR). ERS is thought to be closely linked to oxidative stress and mitochondrial dysfunction, which ultimately cause apoptosis. As a result, ERS regulates apoptosis. Cell proliferation is inhibited as a result of the production of downstream signaling molecules, such as the mitochondrial apoptosis pathway and CHOP (CAAT/enhancer binding protein homologous protein) [1].
In vivo studies on Telomerase-IN-1 are limited, as the compound is primarily used as a research tool for in vitro studies. However, telomerase inhibitors have potential therapeutic applications in cancer treatment, and in vivo efficacy studies have been conducted in mouse xenograft models of cancer. In these studies, telomerase inhibitors have been shown to inhibit tumor growth and induce tumor regression. However, specific in vivo data for Telomerase-IN-1 are not widely available in the published literature. |
| Enzyme Assay |
The in vitro telomerase assay for Telomerase-IN-1 typically involves measuring the inhibition of telomerase activity using the TRAP (Telomeric Repeat Amplification Protocol) assay or other telomerase activity assays. In these assays, cell extracts containing telomerase are incubated with the compound and a telomerase substrate, and telomerase activity is measured by PCR amplification of telomeric repeats. The IC50 value is calculated from dose-response curves. These assays are standard for characterizing telomerase inhibitors.
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| Cell Assay |
Cellular assays for Telomerase-IN-1 are conducted using cancer cell lines that express telomerase. Cells are treated with varying concentrations of the compound, and telomerase activity, telomere length, cell proliferation, and apoptosis are assessed. Telomerase activity is measured using the TRAP assay, and telomere length is measured using Southern blotting or quantitative PCR. Cell proliferation is assessed using MTT or other assays. These cell-based assays confirm the compound's activity as a telomerase inhibitor and provide information about its effects on cancer cells.
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| Animal Protocol |
In vivo animal studies for Telomerase-IN-1 are conducted in mouse xenograft models of cancer. In these studies, immunocompromised mice are implanted with cancer cells, and tumors are allowed to grow to a certain size. Telomerase-IN-1 is administered orally or intraperitoneally at various doses, and tumor growth is monitored. Telomerase activity and telomere length are measured in tumor tissues. These studies confirm the compound's in vivo efficacy and support its potential as a cancer therapeutic.
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| ADME/Pharmacokinetics |
Telomerase-IN-1 has a molecular weight of approximately 363.23 and a molecular formula of C15H11BrN2O2S. The compound is soluble in DMSO for in vitro assays. For research use, Telomerase-IN-1 is typically stored as powder at -20degC for up to 3 years or at 4degC for up to 2 years, and in solvent at -80degC for up to 1 year. Detailed pharmacokinetic parameters such as oral bioavailability, half-life, and tissue distribution have been characterized in preclinical studies for telomerase inhibitors.
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| Toxicity/Toxicokinetics |
Toxicological data for Telomerase-IN-1 are limited. As a research compound, Telomerase-IN-1 has not been systematically evaluated for toxicity in preclinical studies. The compound is for research use only and not for human therapeutic use. Standard safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment. Researchers should consult the Safety Data Sheet (SDS) for specific safety information.
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| References | |
| Additional Infomation |
Telomerase-IN-1 (CAS#: 666859-49-0) is a research compound developed as a potent inhibitor of telomerase for the study of telomere biology and cancer. It has a molecular formula of C15H11BrN2O2S and a molecular weight of approximately 363.23. The compound inhibits telomerase activity, leading to telomere shortening and cancer cell death. Telomerase-IN-1 is not approved for clinical use and is available only for research purposes in oncology and telomere biology.
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| Molecular Formula |
C21H23FN2O4
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| Molecular Weight |
386.416729211807
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| Exact Mass |
386.164
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| CAS # |
666859-49-0
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| PubChem CID |
10475235
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
512.7±50.0 °C at 760 mmHg
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| Flash Point |
263.9±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
3.62
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
517
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC(CN1CCC(CC1)C(=O)C2=CC=C(C=C2)F)C3=CC=C(C=C3)[N+](=O)[O-]
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| InChi Key |
FDXXXOGKSMENLY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23FN2O4/c1-28-20(15-4-8-19(9-5-15)24(26)27)14-23-12-10-17(11-13-23)21(25)16-2-6-18(22)7-3-16/h2-9,17,20H,10-14H2,1H3
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| Chemical Name |
(4-fluorophenyl)-[1-[2-methoxy-2-(4-nitrophenyl)ethyl]piperidin-4-yl]methanone
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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 : ~100 mg/mL (~258.79 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 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 | 2.5879 mL | 12.9393 mL | 25.8786 mL | |
| 5 mM | 0.5176 mL | 2.5879 mL | 5.1757 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5879 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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