2. Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Glyoxalase (GLO) Apoptosis DNA/RNA Synthesis PARP
  4. TLSC702

TLSC702 is a human glyoxalase I (hGLO I) inhibitor with an IC50 of 2.0 μM. TLSC702 inhibits the activity of human glyoxalase I, thereby leading to the accumulation of methylglyoxal and its derived advanced glycation end products. TLSC702 inhibits tumor cell proliferation, induces apoptotic morphological changes, internucleosomal DNA fragmentation and PARP cleavage in tumor cells. TLSC702 can be used in research related to leukemia and lung cancer.

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TLSC702

TLSC702 Chemical Structure

CAS No. : 748786-57-4

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Based on 1 publication(s) in Google Scholar

TLSC702 Related Antibodies

Top Publications Citing Use of Products

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

TLSC702 is a human glyoxalase I (hGLO I) inhibitor with an IC50 of 2.0 μM. TLSC702 inhibits the activity of human glyoxalase I, thereby leading to the accumulation of methylglyoxal and its derived advanced glycation end products. TLSC702 inhibits tumor cell proliferation, induces apoptotic morphological changes, internucleosomal DNA fragmentation and PARP cleavage in tumor cells. TLSC702 can be used in research related to leukemia and lung cancer[1].

In Vitro

TLSC702 (24 h) suppresses the proliferation of human myeloid leukemia HL-60 cells in a dose-dependent manner with an EC50 of approximately 400 μM[1].
TLSC702 (100-1000 μM; 24 h) induces apoptosis in human myeloid leukemia HL-60 cells in a dose-dependent manner, as evidenced by morphological changes, DNA ladder formation, and PARP cleavage, with necrotic cell death also occurring at 1000 μM[1].
TLSC702 (24 h (both cell lines); 24, 48, 72 h (NCI-H522 cells only)) preferentially suppresses the proliferation of GLO I-high human lung cancer NCI-H522 cells compared to GLO I-low human lung cancer NCI-H460 cells, with a time-dependent antiproliferative effect on NCI-H522 cells that yields EC50 values of >300 μM (24 h), 202 μM (48 h), and 145 μM (72 h)[1].
TLSC702 (300 μM; 24, 48, 72 h) induces accumulation of argpyrimidine adducts in human lung cancer NCI-H522 cells[1].

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

TLSC702 Related Antibodies

Apoptosis Analysis[1]

Cell Line: human myeloid leukemia HL-60 cells
Concentration: 100, 300 and 1000 μM
Incubation Time: 24 h
Result: Induced dose-dependent apoptotic morphological changes, including apoptotic bodies at 300 and 1000 μM.
Induced characteristic apoptotic DNA ladder formation in a dose-dependent manner at 300 μM.
Detected dose-dependent cleavage of PARP across tested concentrations.
Detected necrotic cell death at 1000 μM.

Western Blot Analysis[1]

Cell Line: human lung cancer NCI-H522 cells
Concentration: 300 μM
Incubation Time: 24, 48, 72 h
Result: Induced accumulation of argpyrimidine adducts (methylglyoxal-derived advanced glycation end-products) in NCI-H522 cells.
Molecular Weight

325.38

Formula

C18H15NO3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)CC(=CC1=CC=C(OC)C=C1)C2=NC=3C=CC=CC3S2
Shipping

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

DMSO : 50 mg/mL (153.67 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 3.0733 mL 15.3666 mL 30.7333 mL
5 mM 0.6147 mL 3.0733 mL 6.1467 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.25 mg/mL (3.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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 3.0733 mL 15.3666 mL 30.7333 mL 76.8332 mL
5 mM 0.6147 mL 3.0733 mL 6.1467 mL 15.3666 mL
10 mM 0.3073 mL 1.5367 mL 3.0733 mL 7.6833 mL
15 mM 0.2049 mL 1.0244 mL 2.0489 mL 5.1222 mL
20 mM 0.1537 mL 0.7683 mL 1.5367 mL 3.8417 mL
25 mM 0.1229 mL 0.6147 mL 1.2293 mL 3.0733 mL
30 mM 0.1024 mL 0.5122 mL 1.0244 mL 2.5611 mL
40 mM 0.0768 mL 0.3842 mL 0.7683 mL 1.9208 mL
50 mM 0.0615 mL 0.3073 mL 0.6147 mL 1.5367 mL
60 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2806 mL
80 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9604 mL
100 mM 0.0307 mL 0.1537 mL 0.3073 mL 0.7683 mL
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TLSC702 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:

TLSC702748786-57-4TLSC 702TLSC-702Glyoxalase (GLO)ApoptosisDNA/RNA SynthesisPARPpoly ADP ribose polymerasehuman myeloid leukemia HL-60 cellsleukemiahuman lung cancer NCI-H522 cellsmethylglyoxalapoptosisadvanced glycation end-productslung cancerhuman glyoxalase IPARP cleavagehuman lung cancer NCI-H460 cellsInhibitorinhibitorinhibit

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