ST13
ST13, an ortho-hydroxyanilide, is a selective, slow- and tight-binding HDAC1 and HDAC2 inhibitor with IC50s of 23 nM and 49 nM, respectively. ST13 shows a weak inhibition of HDAC3 (IC50 = 4.30 μM) and HDAC6 (IC50 > 10 μM). The induced fit mechanism of ST13 proceeds through a two-step process: first, the enzyme and inhibitor rapidly form a collision complex (EI), which then slowly transforms into the stable complex E*I. ST13 induces apoptosis in cancer cells. ST13 can be used for the study of melanoma and triple-negative breast.
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- CAS 番号: 1013620-98-8
- 分子式: C21H18N2O3
- 分子量:346.38
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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
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HDAC1 23 nM (IC50) |
HDAC2 49 nM (IC50) |
HDAC3 4300 nM (IC50) |
HDAC6 >10 μM (IC50) |
ST13 (72-120 h) exhibits time-dependent antiproliferative activity in cancer cell lines, with EC50 values decreasing from 2.77 µM (72 h) to 0.311 µM (120 h) in MV-3 cells. In MDA-MB-231, EC50 values decreased from 4.87 µM (72 h) to 0.087 µM (120 h)[1].
ST13 (10 µM; 48 h) significantly induces apoptosis in MDA-MB-231 cells[1].
ST13 (5 μM, 24-72 h) shows a substantial increase in acetylated histone H3 in MV-3 cells[1].
In MV-3 cells, MDA-MB-231 cells, nontumorigenic cell line HEK293 and hematological cancer cell line MM.1S, ST13 (18 h) exhibits an inhibitory effect against HDACs, with EC50 values of 0.311 μM, 0.577 μM, 0.333 μM and 0.637 μM, respectively[1].
ST17 (0.040 µM, 0.072 µM; 10 min) is a light-activatable prodrug of ST13 with potent HDAC1/HDAC2 inhibition upon UV irradiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231
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Concentration:10 µM
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Incubation Time:48 h
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Result:Induced apoptosis in MDA-MB-231 cells.
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Cell Line:MV-3 cells
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Concentration:5 µM
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Incubation Time:24 h, 48 h, 72 h
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Result:Only led to hyperacetylation of histone H3, indicating selectivity toward class I HDACs and the absence of HDAC6 inhibition in a cellular environment.
化学情報
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CAS 番号 1013620-98-8
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分子量 346.38
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分子式 C21H18N2O3
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SMILES
CC(NC1=CC=C(C(NC2=C(O)C=CC(C3=CC=CC=C3)=C2)=O)C=C1)=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
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)