TC13172
Based on 3 publication(s) in Google Scholar
TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
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- 純度: 99.04%
- CAS 番号: 2093393-05-4
- 分子式: C17H16N4O5S
- 分子量:388.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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MedChemExpress（MCE）の使用を引用している文献 TC13172
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生物活性
EC50: 2±0.6 nM (MLKL, in HT-29 cells)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | EC50 |
0.006 μM
Compound: TC13172
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Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 24 hrs by CCK8 assay
Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 24 hrs by CCK8 assay
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[PMID: 39180479] |
| HT-29 | EC50 |
0.006 μM
Compound: TC13172
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Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 4 hrs followed by fresh medium replacement without compound by CCK8 assay
Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 4 hrs followed by fresh medium replacement without compound by CCK8 assay
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[PMID: 39180479] |
| HT-29 | EC50 |
2 nM
Compound: TC13172
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Anti-necroptic activity in human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis incubated for 24 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis incubated for 24 hrs by celltiter-glo luminescent cell viability assay
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[PMID: 36136378] |
| HT-29 | EC50 |
2 nM
Compound: 35; TC13172
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Anti-necroptotic activity in human HT-29 cells assessed as reduction in T/S/Z induced necroptosis measured for 24 hrs by CellTiter-Glo assay
Anti-necroptotic activity in human HT-29 cells assessed as reduction in T/S/Z induced necroptosis measured for 24 hrs by CellTiter-Glo assay
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[PMID: 36781172] |
| HT-29 | IC50 |
2 nM
Compound: 68; TC13172
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Anti-neprotic activity in human HT-29 cells assessed as reduction in TSZ-induced necroptosis incubated for 24 hrs by cell titer glo-based luminescence assay
Anti-neprotic activity in human HT-29 cells assessed as reduction in TSZ-induced necroptosis incubated for 24 hrs by cell titer glo-based luminescence assay
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[PMID: 31622096] |
| HT-29 | IC50 |
2.64 μM
Compound: TC13172
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Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
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[PMID: 39180479] |
The anti-necroptosis potency of TC13172 is evaluated in the HT-29 cell line, the EC50 value is 2±0.6 nM. TC13172 has an inhibition potency of 2 nM against cell necroptosis. TC13172 inhibits MLKL by directly binding to Cys-86. TC13172 does not disrupt the phosphorylation of MLKL, but do decrease the level of MLKL in the membrane phase, demonstrating that these MLKL inhibitors block the translocation of MLKL to the cell membrane, thereby protecting cells from necroptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2093393-05-4
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性状 Solid
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分子量 388.40
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分子式 C17H16N4O5S
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Color Off-white to light yellow
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SMILES
O=C1C2=C(N=C(S(C)(=O)=O)N2C)N(CC#CC3=CC(O)=CC=C3)C(N1C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
Necroptosis executioner MLKL plays pivotal roles in agonist-induced platelet prothrombotic responses and lytic cell death in a temporal order. [Abstract]2023 Aug;30(8):1886-1899. PMID: 37301927 -
Cell Rep
Autoinhibitory control of MLKL governs pseudokinase domain phosphorylation and oligomerization during necroptosis. [Abstract]2026 Mar 20;45(4):117130. PMID: 41863805 -
Sci Rep
2023 Feb 22;13(1):3095. PMID: 36813876
溶剤 & 溶解度
DMSO : 25 mg/mL (64.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (5.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
Human colorectal adenocarcinoma (HT)-29 cells are incubated with compound 12 (1 mM) or DMSO for 2 h. For the binding competition experiment samples, cells are pre-incubated with 5 mM NSA or 100 nM TC13172 for 2 h, 1 mM compound 12 is then added and incubated for an additional 2 h. The click reaction (Biotin-C2H4-N3 10 mM, TBTA 10 mM, CuSO4 50 mM, Sodium ascorbate 50 mM) is carried out with cell lysates for 2 h. The biotinmodified proteins are enriched and analysed by western blotting using antibodies against flag and GAPDH[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5747 mL | 12.8733 mL | 25.7467 mL | 64.3666 mL |
| 5 mM | 0.5149 mL | 2.5747 mL | 5.1493 mL | 12.8733 mL | |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5747 mL | 6.4367 mL | |
| 15 mM | 0.1716 mL | 0.8582 mL | 1.7164 mL | 4.2911 mL | |
| 20 mM | 0.1287 mL | 0.6437 mL | 1.2873 mL | 3.2183 mL | |
| 25 mM | 0.1030 mL | 0.5149 mL | 1.0299 mL | 2.5747 mL | |
| 30 mM | 0.0858 mL | 0.4291 mL | 0.8582 mL | 2.1456 mL | |
| 40 mM | 0.0644 mL | 0.3218 mL | 0.6437 mL | 1.6092 mL | |
| 50 mM | 0.0515 mL | 0.2575 mL | 0.5149 mL | 1.2873 mL | |
| 60 mM | 0.0429 mL | 0.2146 mL | 0.4291 mL | 1.0728 mL |
TC13172 関連分類
HY-101524 関連分類
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