HSP70-IN-1
Based on 1 publication(s) in Google Scholar
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
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- 純度: 98.07%
- CAS 番号: 1268273-90-0
- 分子式: C24H28N6O2S
- 分子量:464.58
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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
MedChemExpress(MCE)の使用を引用している文献 HSP70-IN-1
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生物活性
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HSP70 |
Caspase-3/7 1.9 μM (IC50, MOLM13 cells) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Kasumi 1 | IC50 |
2.3 μM
Compound: 27c
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Cytotoxicity against human Kasumi-1 cells after 72 hrs by alamar blue assay
Cytotoxicity against human Kasumi-1 cells after 72 hrs by alamar blue assay
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[PMID: 24548239] |
| MOLM-13 | IC50 |
1.9 μM
Compound: 27c
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Induction of apoptosis in human MOLM13 cells assessed as caspase 3/7 activation after 16 hrs by fluorescence assay
Induction of apoptosis in human MOLM13 cells assessed as caspase 3/7 activation after 16 hrs by fluorescence assay
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[PMID: 24548239] |
The heat shock protein 70 (Hsp70) is a molecular chaperone which plays an important function in protein homeostasis as well as in cell signaling and survival. Hsp70 is frequently overexpressed in cancer, where the elevated expression is furthermore believed to be a cause of or to lead to resistance to chemotherapy and other treatments. HSP70-IN-1 interferes with the formation of functional Hsp70-HOP-Hsp90 machinery by its ability to dose-dependently alter the megacomplex components and to destabilize an Hsp70-Hsp90 machinery client, Raf-1. In cells, the refolding of heat-denatured luciferase by endogenous as well as transfected Hsp70 is inhibited by HSP70-IN-1. HSP70-IN-1 also results in induction of apoptosis in cancer cells. Addition of HSP70-IN-1to cancer cells dose-dependently alters the formation of the Hsp70-HOP complex, a phenomenon associated with their destabilization and reduction in half-life[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 1268273-90-0
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性状 Solid
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分子量 464.58
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分子式 C24H28N6O2S
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CC(SC2=CN=C(N3CCN(C)CC3)N=C2OCC4=CC=CC=C4)=C1)CN
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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 (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : 50 mg/mL (107.62 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: ≥ 2.5 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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 (271 KB)
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SDS (393 KB)
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- Portuguese - PT (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 | 2.1525 mL | 10.7624 mL | 21.5248 mL | 53.8120 mL |
| 5 mM | 0.4305 mL | 2.1525 mL | 4.3050 mL | 10.7624 mL | |
| 10 mM | 0.2152 mL | 1.0762 mL | 2.1525 mL | 5.3812 mL | |
| 15 mM | 0.1435 mL | 0.7175 mL | 1.4350 mL | 3.5875 mL | |
| 20 mM | 0.1076 mL | 0.5381 mL | 1.0762 mL | 2.6906 mL | |
| 25 mM | 0.0861 mL | 0.4305 mL | 0.8610 mL | 2.1525 mL | |
| 30 mM | 0.0717 mL | 0.3587 mL | 0.7175 mL | 1.7937 mL | |
| 40 mM | 0.0538 mL | 0.2691 mL | 0.5381 mL | 1.3453 mL | |
| 50 mM | 0.0430 mL | 0.2152 mL | 0.4305 mL | 1.0762 mL | |
| 60 mM | 0.0359 mL | 0.1794 mL | 0.3587 mL | 0.8969 mL | |
| 80 mM | 0.0269 mL | 0.1345 mL | 0.2691 mL | 0.6727 mL | |
| 100 mM | 0.0215 mL | 0.1076 mL | 0.2152 mL | 0.5381 mL |