LCS-1
Based on 3 publication(s) in Google Scholar
LCS-1 is a superoxide dismutase 1 (SOD1) inhibitor. LCS-1 inhibits SOD1 activity with an IC50 value of 1.07 μM. LCS-1 induces the early- and late-stage apoptosis of multiple myeloma (MM.1S) cells.
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- 純度: 99.81%
- CAS 番号: 41931-13-9
- 分子式: C11H8Cl2N2O
- 分子量:255.10
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Apoptosis Compound Library
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MedChemExpress（MCE）の使用を引用している文献 LCS-1
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生物活性
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SOD1 1.07 μM (IC50) |
LCS-1 (1-10000 nM; 24 hours) has selective cytotoxicity towards bloom syndrome gene product (BLM) -proficient and BLM-deficient HCT116 cells[1].
LCS-1 shows growth inhibitory effect on 10/27 adenocarcinoma cell lines (median IC50=0.20 μM; such as H23, H2347, HCC827 cell lines) and normal human bronchial epithelial (NHBE) cells (IC50=2.66 μM)[2].
LCS-1 (0, 1.25, 2 μM; 4 h) in a concentration-dependent manner triggers significant inhibition of SOD1 enzymatic activity in multiple myeloma (MM) cells[3].
LCS-1 (0, 1.25, 2.5, 5 μM; 48 h) in a dose-dependent manner reduces the viability of various MM cell lines, including MM.1R (Dexamethasone-resistant), Dox40 (Doxorubicin-resistant), or LR5 (Melphalan-resistant) cell lines[3].
LCS-1 (48 h) has IC50 values of 2.5 and 4.6 μM for cell viability of ANBL6-WT (Bortezomib-sensitive) and ANBL6-BR (Bortezomib- resistant) cells, respectively[3].
LCS-1 (1.25 μM; 16 h) induces a significant increase in ROS levels and O2 levels in MM.1S cells[3].
LCS-1 (1.25 μM; 16 h) shows a significant decrease in GSH/GSSG ratio in MM.1S cells[3].
LCS-1 (1.25 μM; 24h) induces the release of mitochondrial cytochrome-c into the cytosol, and enriches the proteins (HSP60/CLPP) mediating mtUPR signaling in MM.1S cells[3].
LCS-1-induced O2 (1.25 μM; 5 h) triggers a marked decrease in both RP2CP and RP1CP forms of 26S proteasomes[3].
LCS-1 (2 μM; 16 h) induces the early- and late-stage apoptosis of MM.1S cells[3].
LCS-1 (0, 0.5, 1, 1.5, 2 μM) upregulates p53/p21 signaling, as well as downregulates survival pathway proteins MCL-1, BclxL, or c-Myc in MM.1S cells[3].
LCS-1 (0, 4, 8, 16, 24 h; 2 μM) shows a rapid and robust induction of mitochondrial unfolded protein response (UPR) proteins (BIP, PERK, phosphorylated eIF2α, or a lectin protein calnexin) in MM.1S and ANBL6-BR cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BLM-proficient and BLM-deficient HCT116 cells
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Concentration:1-10000 nM
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Incubation Time:24 hours
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Result:Had IC50 values of 1462 nM and 24.92 nM for the viability of BLM-proficient and BLM-deficient HCT116 cells, respectively.
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Cell Line:MM.1S and ANBL6-BR cells
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Concentration:2 μM
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Incubation Time:16 hours
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Result:Decreased the expression of cell-cycle regulatory proteins (cyclin-B1, CDC25C, and CDC2).
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Cell Line:MM.1S cells
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Concentration:0, 0.5, 1, 1.5, 2 μM
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Incubation Time:
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Result:Upregulated p53/p21 signaling, as well as downregulated survival pathway proteins MCL-1, BclxL, or c-Myc.
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Cell Line:MM.1S cells
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Concentration:2 μM
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Incubation Time:0, 4, 8, 16, 24 hours
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Result:Showed a rapid and robust induction of UPR proteins (BIP, PERK, phosphorylated eIF2α, or a lectin protein calnexin).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-week-old female CB17 SCID mice (MM.1S tumors volume=100 mm3)[3]
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Dosage:20 mg/kg (diluted in saline)
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Administration:Intraperitoneal injections; treated on an every other day schedule for 14 days
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Result:Inhibited MM growth and prolongs host survival.
化学情報
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CAS 番号 41931-13-9
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性状 Solid
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分子量 255.10
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分子式 C11H8Cl2N2O
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Color Light yellow to light brown
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SMILES
O=C1C(Cl)=C(Cl)C=NN1C2=CC=CC(C)=C2
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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 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Drug Resist Updat
CRISPR/Cas9 screens unravel miR-3689a-3p regulating sorafenib resistance in hepatocellular carcinoma via suppressing CCS/SOD1-dependent mitochondrial oxidative stress. [Abstract]2023 Nov:71:101015. PMID: 37924725 -
Exp Cell Res
A novel molecular target, superoxide dismutase 1, in ALK inhibitor-resistant lung cancer cells, detected through proteomic analysis. [Abstract]2024 Oct 1;442(2):114266. PMID: 39313177 -
溶剤 & 溶解度
DMSO : 50 mg/mL (196.00 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, 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.
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.
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.
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.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (419 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gupta A, et al. Nanocarrier Composed of Magnetite Core Coated with Three Polymeric Shells Mediates LCS-1 Delivery for Synthetic Lethal Therapy of BLM-Defective Colorectal Cancer Cells. Biomacromolecules. 2018 Mar 12;19(3):803-815. [Content Brief]
[2]. Somwar R, et al. Superoxide dismutase 1 (SOD1) is a target for a small molecule identified in a screen for inhibitors of the growth of lung adenocarcinoma cell lines. Proc Natl Acad Sci U S A. 2011;108(39):16375-16380. [Content Brief]
[3]. Du T, et al. Proteomic analysis identifies mechanism(s) of overcoming bortezomib resistance via targeting ubiquitin receptor Rpn13. Leukemia. 2021 Feb;35(2):550-561. [Content Brief]
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 | 3.9200 mL | 19.6002 mL | 39.2003 mL | 98.0008 mL |
| 5 mM | 0.7840 mL | 3.9200 mL | 7.8401 mL | 19.6002 mL | |
| 10 mM | 0.3920 mL | 1.9600 mL | 3.9200 mL | 9.8001 mL | |
| 15 mM | 0.2613 mL | 1.3067 mL | 2.6134 mL | 6.5334 mL | |
| 20 mM | 0.1960 mL | 0.9800 mL | 1.9600 mL | 4.9000 mL | |
| 25 mM | 0.1568 mL | 0.7840 mL | 1.5680 mL | 3.9200 mL | |
| 30 mM | 0.1307 mL | 0.6533 mL | 1.3067 mL | 3.2667 mL | |
| 40 mM | 0.0980 mL | 0.4900 mL | 0.9800 mL | 2.4500 mL | |
| 50 mM | 0.0784 mL | 0.3920 mL | 0.7840 mL | 1.9600 mL | |
| 60 mM | 0.0653 mL | 0.3267 mL | 0.6533 mL | 1.6333 mL | |
| 80 mM | 0.0490 mL | 0.2450 mL | 0.4900 mL | 1.2250 mL | |
| 100 mM | 0.0392 mL | 0.1960 mL | 0.3920 mL | 0.9800 mL |
LCS-1 関連分類
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