2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. GTSE1-IN-1

GTSE1-IN-1 is an orally active GTSE1 inhibitor. GTSE1-IN-1 can suppress GTSE1 transcription and expression. GTSE1-IN-1 can inhibit cancer cell proliferation by inducing cell cycle arrest and cell senescence through the persistence of DNA damage. GTSE1-IN-1 can be used for the research of cancer, such as colon and lung cancer.

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

GTSE1-IN-1

GTSE1-IN-1 Chemical Structure

CAS No. : 3002034-34-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Based on 1 publication(s) in Google Scholar

GTSE1-IN-1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GTSE1-IN-1 is an orally active GTSE1 inhibitor. GTSE1-IN-1 can suppress GTSE1 transcription and expression. GTSE1-IN-1 can inhibit cancer cell proliferation by inducing cell cycle arrest and cell senescence through the persistence of DNA damage. GTSE1-IN-1 can be used for the research of cancer, such as colon and lung cancer[1].

In Vitro

GTSE1-IN-1 (Compound Y18) (0.5-2 μM, 48 h) inhibits the proliferation of HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 7 days) reduces the number of colony formation in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) induces G2/M phase arrest[1].
GTSE1-IN-1 (0.5-2 μM, 4 days) induces cell senescence in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) induces extensive DNA damage in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) reduces cell adhesion, migration and invasion in HCT116 and A549 cells[1].
GTSE1-IN-1 (0.5-2 μM, 48 h) inhibits the transcription and protein expression of GTSE1 in HCT116 and A549 cells[1].

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

GTSE1-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HCT116 and A549 cells
Concentration: 0.5, 1 and 2 μM
Incubation Time: 48 h
Result: Increased cells in G2/M phase.
Decreased the expression of G2/M phase-related proteins cyclin B1 and CDC2.
In Vivo

GTSE1-IN-1 (Compound Y18) (15-30 mg/kg, i.p., every other day for 28 days) inhibits tumor growth in HCT116-derived xenograft tumor mice models[1].

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

Animal Model: HCT116-derived xenograft tumor mice models[1]
Dosage: 15 and 30 mg/kg
Administration: Intraperitoneally injection, every other day for 28 days
Result: Reduced tumor volume.
Decreased the expression of GTSE1 and proliferation marker Ki67 in tumor tissues.
Increased the expression of DNA damage marker γ-H2AX.
Had no effect on body weight and liver/kidney function.
Molecular Weight

393.46

Formula

C21H24FN7
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CN=C(NC2=CC=C(N3CCN(C)CC3)C=C2)N=C1NC4=CC=C(N)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (254.16 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 2.5416 mL 12.7078 mL 25.4155 mL
5 mM 0.5083 mL 2.5416 mL 5.0831 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. 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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: 98.07%

SDS (251 KB)

COA (250 KB) HNMR (276 KB) LCMS (104 KB)

Handling Instructions (2659 KB)
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5416 mL 12.7078 mL 25.4155 mL 63.5389 mL
5 mM 0.5083 mL 2.5416 mL 5.0831 mL 12.7078 mL
10 mM 0.2542 mL 1.2708 mL 2.5416 mL 6.3539 mL
15 mM 0.1694 mL 0.8472 mL 1.6944 mL 4.2359 mL
20 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1769 mL
25 mM 0.1017 mL 0.5083 mL 1.0166 mL 2.5416 mL
30 mM 0.0847 mL 0.4236 mL 0.8472 mL 2.1180 mL
40 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5885 mL
50 mM 0.0508 mL 0.2542 mL 0.5083 mL 1.2708 mL
60 mM 0.0424 mL 0.2118 mL 0.4236 mL 1.0590 mL
80 mM 0.0318 mL 0.1588 mL 0.3177 mL 0.7942 mL
100 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6354 mL
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GTSE1-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:

GTSE1-IN-13002034-34-3DNA/RNA SynthesisGTSE1DNAHCT116A549Colon cancerLung cancerInhibitorinhibitorinhibit

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