Telomerase-IN-1

Cat. No.: HY-U00268 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

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Telomerase-IN-1 is a Telomerase inhibitor with an IC₅₀ of 0.19 μM.

For research use only. We do not sell to patients.

Telomerase-IN-1 Chemical Structure

CAS No. : 666859-49-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 275	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 275	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Protocol
Purity & Documentation
References
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Description

Telomerase-IN-1 is a Telomerase inhibitor with an IC₅₀ of 0.19 μM.

IC₅₀ & Target

IC50: 0.19 μM (Telomerase) ^[1]

In Vitro

Our in vitro studies show that title compound (Telomerase-IN-1) has high inhibitory activity against telomerase and high antiproliferative capacity on SMMC-7721 cells, and has no obvious toxic effect on human normal hepatocyte cells. Telomerase-IN-1 treatment decreases the growth of cancer cells in dose- and time-dependent manners; however, the viability of L-02 shows slight changes in the compound at 10 μM. 48 h of SMMC-7721 cell treatment with the Telomerase-IN-1 (20, 40, and 80 nM) causes increase of apoptosis. Forty-eight hours of SMMC-7721 cell treatment with the Telomerase-IN-1(20, 40, and 80 nM) causes significant accumulation of green fluorescence, indicating a decrease in MMP. At 40 nM, Telomerase-IN-1 significantly increases expressions of cyt-c and Bax, but the Bcl-2 level is decreased^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Our in vivo studies show that this compound (Telomerase-IN-1) significantly inhibits tumor growth in xenograft tumor models. Results show that endoplasmic reticulum stress (ERS) through ER over response (EOR) activates the expression of hTERT, and then induces ERS, which is believed to be intricately associated with oxidative stress and mitochondrial dysfunction, resulting in apoptotic cell death, thereby modulating the expression of downstream signaling molecules including CHOP (CAAT/enhancer-binding protein homologous protein)) and mitochondrion pathway of apoptosis, leading to inhibition of cell proliferation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

386.42

Formula

C₂₁H₂₃FN₂O₄

CAS No.

666859-49-0

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=C(F)C=C1)C2CCN(CC(OC)C3=CC=C([N+]([O-])=O)C=C3)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (258.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (248 KB) HNMR (254 KB) RP-HPLC (368 KB) MS (108 KB)

Handling Instructions (2659 KB)

References

[1]. Cheng X, et al. Discovery of (4-bromophenyl)(3-hydroxy-4-methoxyphenyl)methanone through upregulating hTERT induces cell apoptosis and ERS. Cell Death Dis. 2017 Aug 24;8(8):e3016. [Content Brief]

Cell Assay ^[1]	The effect of the title compound (Telomerase-IN-1) on the viability of human hepatoma cancer cell (SMMC-7721) is examined by increasing concentrations (3.2, 16, 80, 400, and 2000 nM). A normal liver cell line (L-02) is used as control. Cell viability is measured by MTTassay at 48 h^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	To test whether the Telomerase-IN-1 shows any antitumor effect in vivo, SMMC-7721 cells are xenografted into nude mice, and then the tumor-bearing animals are treated with the Telomerase-IN-1 (25, 50, and 100 μM/daily) for 37 days by intraperitoneal injection^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Cheng X, et al. Discovery of (4-bromophenyl)(3-hydroxy-4-methoxyphenyl)methanone through upregulating hTERT induces cell apoptosis and ERS. Cell Death Dis. 2017 Aug 24;8(8):e3016. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5879 mL	12.9393 mL	25.8786 mL	64.6964 mL
	5 mM	0.5176 mL	2.5879 mL	5.1757 mL	12.9393 mL
	10 mM	0.2588 mL	1.2939 mL	2.5879 mL	6.4696 mL
	15 mM	0.1725 mL	0.8626 mL	1.7252 mL	4.3131 mL
	20 mM	0.1294 mL	0.6470 mL	1.2939 mL	3.2348 mL
	25 mM	0.1035 mL	0.5176 mL	1.0351 mL	2.5879 mL
	30 mM	0.0863 mL	0.4313 mL	0.8626 mL	2.1565 mL
	40 mM	0.0647 mL	0.3235 mL	0.6470 mL	1.6174 mL
	50 mM	0.0518 mL	0.2588 mL	0.5176 mL	1.2939 mL
	60 mM	0.0431 mL	0.2157 mL	0.4313 mL	1.0783 mL
	80 mM	0.0323 mL	0.1617 mL	0.3235 mL	0.8087 mL
	100 mM	0.0259 mL	0.1294 mL	0.2588 mL	0.6470 mL

Telomerase-IN-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Telomerase-IN-1666859-49-0TelomeraseInhibitorinhibitorinhibit

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