HDAC-IN -45 (Compound 14) 是一种小分子HDAC抑制剂，具有抗癌活性，也可与 Y303 残基形成氢键。HDAC-IN-45 (Compound 14) 对 HDAC1、2 和 3 亚型具有显著的抑制作用，IC50分别为 0.108、0.585 和 0.563 μM。
| 生物活性 | HDAC-IN-45 (Compound 14) is a small moleculeHDACinhibitor and has anticancer activity, also can forms a hydrogen
bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towardsHDAC1, 2 and 3 isoforms withIC50values of 0.108, 0.585 and 0.563 μM respectively[1]. |
| IC50& Target[1] | HDAC1 0.108 μM (IC50) | HDAC2 0.585 μM (IC50) | HDAC3 0.563 μM μM (IC50) | HDAC6 ﹥10 μM (IC50) | HDAC8 6.81 μM (IC50) |
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体外研究
(In Vitro) | HDAC-IN-45 (Compound 14) suppresses the growth of triple-negative breast cancer cells MDA-MB-231 (IC50= 1.48 μM), MDA-MB-468 (IC50= 0.65 μM), and liver cancer cells HepG2 (IC50= 2.44 μM).
HDAC-IN-45 has equally virulent in the HDAC-sensitive cell lines (YCC11) and -resistant gastric cell lines (YCC3/7) and overcome HDACi resistance. HDAC-IN-45 has a high toxicity (IC50= 0.33 μM) in three leukemic cell lines, K-562, KG-1 and THP-1.
HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms withIC50values of 0.108, 0.585 and 0.563 μM respectively.
HDAC-IN-45 (Compound 14) can elevate acetylation level of histone H3 and expression of p21.
HDAC-IN-45 (Compound 14) exerts a dose-dependent upregulation of ac-H3K9 in MDA-MB-231 cells, triggers cell cycle arrest in G1 phase.
HDAC-IN-45 (Compound 14) exhibits a potent antitumor efficacy in xenograft mouse model[1].
Cell Proliferation Assay[1] | Cell Line: | Triple-negative breast cancer cells; liver cancer cells; YCC11 and YCC3/7 | | Concentration: | a series of concentration | | Incubation Time: | 72 h | | Result: | Inhibited the cell growth viability of HepG2 and triple-negative breast cancer cells. |
Cell Cytotoxicity Assay[1] | Cell Line: | Three leukemic cell lines (K-562, KG-1 and THP-1); YCC3/7 and YCC11 cell lines | | Concentration: | a series of concentration | | Incubation Time: | 72 h | | Result: | Showed a potent anti-cancer effect, exhibited high sensitivities and strong toxicities with IC50 values below micromolar in leukemic cell lines. |
Western Blot Analysis[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 2 μM | | Incubation Time: | 24 h | | Result: | Elevated acetylation level of histone H3 and expression of p21. |
Cell Cycle Analysis[1] | Cell Line: | MDA-MB-231cells | | Concentration: | 4 μM | | Incubation Time: | 24 h | | Result: | Arrested cell cycle in G1 and trigger apoptosis. |
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体内研究
(In Vivo) | HDAC-IN-45 (Compound 14) (25 mg/kg or 50mg/kg; i.p.; every day) exhibits a potent antitumor efficacy in human MDA-MB-231 breast cancer xenograft mouse model[1].
| Animal Model: | Human MDA-MB-231 breast cancer xenograft mouse model[1] | | Dosage: | 25 mg/kg or 50mg/kg | | Administration: | 25 mg/kg or 50mg/kg; i.p.; every day. | | Result: | Exhibited a potent antitumor efficacy. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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