HDAC1-IN-14
HDAC1-IN-14 is an indole-based benzamide selective HDAC1 inhibitor with an IC50 of 77 nM. HDAC1-IN-14 acts as an antiproliferative agent, with GI50 values ranging from nanomolar to low micromolar levels in various cancer cells. HDAC1-IN-14 induces G0-G1 cell cycle arrest in colon cancer cells. HDAC1-IN-14 upregulates the expression of Caspase-3, Cyto-C and Bax, and downregulates the expression of AKT-1. HDAC1-IN-14 can be used in research related to leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer.
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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。
- 分子式: C30H26N4O3
- 分子量:490.55
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
[1]|
HDAC1 77 nM () |
体外実験
HDAC1-IN-14 (Compound 23c) at 10 μM potently inhibits the growth of NCI-60 tumor cell lines covering multiple cancer types, with a mean GI50 of 1 μM, and exhibits the strongest activity against leukemia cell lines[1].
HDAC1-IN-14 inhibits the proliferation of HCT-116 colon cancer cells with an IC50 of 3 μM[1].
HDAC1-IN-14 (3 μM; 24 h) induces G0-G1 cell cycle arrest in HCT-116 colon cancer cells, with 89.42% of cells arrested at the G0-G1 phase[1].
HDAC1-IN-14 (3 μM; 24 h) regulates the expression of key apoptosis pathway genes in HCT-116 colon cancer cells, including upregulating the expression of pro-apoptotic proteins Caspase-3, Cyto-C and Bax, and downregulating the expression of AKT-1[1].
HDAC1-IN-14 (3 μM; 24 h) inhibits total cellular HDAC activity by 5% in HCT-116 colon cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colon cancer cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Induced G0-G1 phase cell cycle arrest, with 89.42% of cells in the G0-G1 phase, 3.86% in the S phase, 0.01% in the G2-M phase, and 2.35% in the Sub G0-G1 phase.
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Cell Line:HCT-116 colon cancer cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Induced overexpression of Caspase-3 (3-fold), Cyto-C (3-fold), and Bax (16-fold).
Downregulated AKT-1 (0.6-fold).
Showed no significant effect on Bcl-2 expression (2-fold).
Resulted in a Bax/Bcl-2 ratio of 8.
化学情報
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分子量 490.55
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分子式 C30H26N4O3
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SMILES
COC1=CC=C(C(NC2=CC=C(N(CC3=CC=C(C(NC4=CC=CC=C4N)=O)C=C3)C=C5)C5=C2)=O)C=C1
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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)