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| Targets |
Telomerase ( IC50 = 0.89 µM )
Telomerase-IN-2 targets telomerase, the enzyme responsible for maintaining telomere length in cancer cells. The compound inhibits telomerase activity by decreasing the expression of dyskerin, a protein essential for telomerase function. Dyskerin is a component of the telomerase complex, and its reduced expression leads to impaired telomerase activity and telomere shortening. The compound's mechanism involves modulation of the IRE1/XBP1s pathway. By inhibiting telomerase, Telomerase-IN-2 induces telomere shortening and limits the proliferative capacity of cancer cells. |
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| ln Vitro |
Telomerase-IN-2 demonstrates potent in vitro activity with an IC50 of 0.89 μM against telomerase. It exhibits high activity against multiple cancer cell lines in anticancer activity assays, including HeLa, SMMC-7721, SGC-7901, U87, and HepG2. The compound's ability to inhibit telomerase activity and induce telomere shortening makes it a valuable tool for studying telomerase biology and cancer therapeutics. The compound shows potent inhibitory activity by decreasing dyskerin expression.
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| ln Vivo |
In vivo studies for Telomerase-IN-2 have not been extensively documented in the available literature. The compound is primarily used in in vitro research for studying telomerase inhibition and cancer cell proliferation. As a telomerase inhibitor, it has potential for in vivo applications in cancer therapy. Studies in appropriate animal models would be needed to evaluate its in vivo efficacy, pharmacokinetics, and safety profile. The compound's small molecule properties suggest potential for oral bioavailability and tumor penetration.
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| Enzyme Assay |
For telomerase activity assays, Telomerase-IN-2 is tested against telomerase enzyme preparations at various concentrations. Telomerase activity is measured using standard telomerase repeat amplification protocol (TRAP) assays, and IC50 values are calculated from dose-response curves. For cellular studies, cancer cell lines are treated with the compound and telomerase activity, telomere length, and cell proliferation are assessed. Dyskerin expression levels are measured by Western blot or qRT-PCR.
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| Cell Assay |
For cellular studies, cancer cell lines such as HeLa, SMMC-7721, SGC-7901, U87, and HepG2 are cultured in appropriate media and treated with Telomerase-IN-2 at various concentrations. Cells are incubated for 24-72 hours, and cell viability is assessed using MTT or similar assays to determine IC50 values. Telomerase activity is measured using TRAP assays. Telomere length is assessed by Southern blot or quantitative PCR. Dyskerin expression is evaluated by Western blot or qRT-PCR. Apoptosis and cell cycle analysis are performed using flow cytometry.
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| Animal Protocol |
For in vivo studies, appropriate animal models of cancer would be used to evaluate Telomerase-IN-2. The compound would be administered via oral or intraperitoneal routes at various doses. Tumor volume would be measured, and body weight monitored for toxicity. Telomerase activity and telomere length in tumor tissues would be assessed. Pharmacokinetic parameters including half-life, clearance, and tissue distribution would be determined. However, detailed in vivo protocols for Telomerase-IN-2 have not been extensively reported in the literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Telomerase-IN-2 have not been fully characterized in the available literature. The compound has a molecular weight of 633.69 and a molecular formula of C34H39N3O9. It is soluble in DMSO at 250 mg/mL (394.51 mM). The compound should be stored at -20°C, with stability of ≥2 years. Shipping is typically with ice packs. Purity is >98% by HPLC. The compound's IUPAC name is 5,7-dimethoxy-3-{4-[4-(pyridine-4-carbonyl)piperazin-1-yl]butoxy}-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one.
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| Toxicity/Toxicokinetics |
Telomerase-IN-2 is a research compound intended for laboratory use only and is not approved for human therapeutic use. As a telomerase inhibitor with an IC50 of 0.89 μM, it has anticancer activity. The compound shows potent inhibitory activity against telomerase by decreasing dyskerin expression. Standard laboratory safety precautions should be followed when handling this compound. The compound is for research use only and not for human or animal clinical diagnosis.
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| References | |
| Additional Infomation |
Telomerase-IN-2 is a potent small-molecule telomerase inhibitor with molecular formula C34H39N3O9 and molecular weight 633.69. It inhibits telomerase activity by decreasing dyskerin expression with an IC50 of 0.89 μM. The compound exhibits anticancer activity against HeLa, SMMC-7721, SGC-7901, U87, and HepG2 cell lines. It is for research use only and has not been approved for clinical applications. Storage at -20°C is recommended.
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| Molecular Formula |
C34H39N3O9
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|---|---|
| Molecular Weight |
633.688169717789
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| Exact Mass |
633.27
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| CAS # |
1610878-54-0
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| PubChem CID |
76285870
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
46
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C(C2C(=CC(=CC=2OC=1C1C=C(C(=C(C=1)OC)OC)OC)OC)OC)=O)CCCCN1CCN(C(C2C=CN=CC=2)=O)CC1
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| InChi Key |
HDOUAPSDPPFIGT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H39N3O9/c1-40-24-20-25(41-2)29-26(21-24)46-31(23-18-27(42-3)32(44-5)28(19-23)43-4)33(30(29)38)45-17-7-6-12-36-13-15-37(16-14-36)34(39)22-8-10-35-11-9-22/h8-11,18-21H,6-7,12-17H2,1-5H3
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| Chemical Name |
5,7-dimethoxy-3-[4-[4-(pyridine-4-carbonyl)piperazin-1-yl]butoxy]-2-(3,4,5-trimethoxyphenyl)chromen-4-one
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| Synonyms |
Telomerase-IN-2
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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 : ~250 mg/mL (~394.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.28 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 20.8 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: ≥ 2.08 mg/mL (3.28 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 20.8 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 | 1.5781 mL | 7.8903 mL | 15.7806 mL | |
| 5 mM | 0.3156 mL | 1.5781 mL | 3.1561 mL | |
| 10 mM | 0.1578 mL | 0.7890 mL | 1.5781 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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