HDAC-IN-101
HDAC-IN-101 is a HDAC1 inhibitor and nitroreductase/pH-activated fluorescent inducer, with an IC50 of 65 nM against human HDAC1. HDAC-IN-101 blocks cancer cell proliferation by inhibiting HDAC1. HDAC-IN-101 is reduced by overexpressed nitroreductase to generate H6AQ (Ex/Em = 450 nm/500 nm), a product that emits fluorescence under low pH conditions. HDAC-IN-101 is applicable for cancer-related research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1616863-09-2
- 分子式: C25H19N5O4
- 分子量:453.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
1.41 μM
Compound: 12h
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Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
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[PMID: 29288941] |
体外実験
1. Stock Solution Preparation
1.1 Solvent: For most dyes, organic solvents such as anhydrous DMSO are typically used for dissolution.
1.2 Concentration Recommendation: Generally, a high concentration of 1-10 mM stock solution is recommended.
1.3 Storage Conditions: Store at -20 ℃ or -80 ℃ protected from light and avoid repeated freeze-thaw cycles.
2. Working Solution Preparation
2.1 Diluent: Serum-free culture medium or PBS is typically used. Proteins and esterases in serum may interfere with staining or cause dye hydrolysis.
2.2 Working Concentration: 1-10 μM
Note: Please adjust the dye working solution concentration according to your actual situation and prepare fresh before use.
3. Cell Staining
3.1 Culture cells on sterile coverslips.
3.2 Remove the coverslips from the culture medium and aspirate excess medium.
3.3 Add working solution, gently shake to completely cover the cells, and incubate at 37 ℃ for 2-6 h.
3.4 Aspirate the dye working solution, wash 2-3 times with culture medium, 5 minutes each time, and observe using a fluorescence microscope or flow cytometry.
Note: If flow cytometry is required, the cells should be resuspended with trypsin before staining.
HDAC-IN-101 (1 μM; 0-4 h) selectively activates fluorescence in HeLa cells with high NTR expression, showing time-dependent enhancement over 4 h of incubation, while displaying minimal fluorescence in LO2 cells[1].
HDAC-IN-101 (5 μM) is pH independent, displaying minimal fluorescence intensity across pH 4.33 to 7.40 at a concentration of 5 μM when excited at 450 nm[1].
HDAC-IN-101 (5 μM; 0-6 h) is activated by 10 μg/mL NTR and 500 μM NADH at pH 4.00, showing time-dependent fluorescence enhancement at 500 nm over 6 h of incubation[1].
HDAC-IN-101 (Compound H6M) potently inhibits purified HDAC1 enzyme with an IC50 of 65 nM[1].
HDAC-IN-101 (H6M) shows high selectivity for NTR and low pH (4.00), exhibiting significant fluorescence enhancement at 500 nm only when treated with 10 μg/mL NTR and 500 μM NADH at pH 4.00[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6 weeks old)[1]
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Dosage:40 mg/kg
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Administration:i.v.; single dose
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Result:Detected bright fluorescence specifically at the tumor site, with minimal signal at non-target sites.
Confirmed significantly more intense fluorescent signal in tumors than in major organs, with a tumor-to-normal tissue ratio ranging from 3.17 to 12.09.
Enabled clear identification of tumor margins to guide successful tumor resection.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
化学情報
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CAS 番号 1616863-09-2
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分子量 453.45
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分子式 C25H19N5O4
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SMILES
O=C(C1=CC=C(C=C1)CNC2=CC3=C(C(C4=CC=C(C=C4)[N+]([O-])=O)=N2)NC5=C3C=CC=C5)NO
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)