HDAC-IN-47 是一种具有口服活性的组蛋白去乙酰化酶 (HDAC) 的抑制剂，IC50分别为 19.75 nM (HDAC1)，5.63 nM (HDAC6)，40.27 nM (HDAC3)，57.8 nM (HDAC2)，302.73 nM (HDAC8)。HDAC-IN-47 能抑制细胞自噬，并通过Bax/Bcl-2和caspase-3通路诱导凋亡 (apoptosis)。HDAC-IN-47 能够在G2/M期阻滞细胞周期，并在体内表现出抗肿瘤作用。
| 生物活性 | HDAC-IN-47 is an orally active inhibitor ofhistone deacetylase(HDAC), withIC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibitsautophagyand inducesapoptosisvia theBax/Bcl-2andcaspase-3pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo[1]. |
| IC50& Target[1] | HDAC1 19.75 nM (IC50) | HDAC6 5.63 nM (IC50) | HDAC3 40.27 nM (IC50) | HDAC2 57.8 nM (IC50) | HDAC8 302.73 nM (IC50) |
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体外研究
(In Vitro) | HDAC-IN-47 (compound 21) shows antiproliferative activity and inhibits A549 cell growth with an IC50value of 0.24 μM[1].
HDAC-IN-47 (0.5 and 1 μM; 72 h) exhibits profound G2/M arrest in A549 cells and induces cell apoptosis[1].
HDAC-IN-47 (0.1 and 0.5 μM; 24 h) increases the expression levels of Bax and Caspase3, decreases the level of Bcl-2, activates the intrinsic (mitochondrial) apoptotic pathway[1].
Cell Viability Assay[1] | Cell Line: | HepG2, MDA-MB-238, HL-60 cells | | Concentration: | 0.16-0.45 μM | | Incubation Time: | 72 hours | | Result: | Inhibited cancer cells with IC50s of 0.16 μM (HepG2), 0.45 μM (MDA-MB-238), 0.22 μM (HL-60), respectively. |
Cell Cycle Analysis[1] | Cell Line: | A549 cells | | Concentration: | 0.5 and 1 μM | | Incubation Time: | 24 hours | | Result: | Induced marked arrest of cells in the G2/M phase of 28.38% (0.5 μM) and 31.70% (1.0 μM). |
Apoptosis Analysis[1] | Cell Line: | A549 cells | | Concentration: | 0.5 and 1 μM | | Incubation Time: | 24 hours | | Result: | Resulted 21.09% (0.5 μM) and 30.58% (1 μM) apoptotic cells. |
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体内研究
(In Vivo) | HDAC-IN-47 (compound 21) (50, and 100 mg/kg; p.o.; once daily; 18 d) exhibits significant antitumor activity in a dosedependent manner without no significant body weight loss in A549 xenograft mouse model[1].
| Animal Model: | A549 xenograft model in mouse (female, BALB/c nu/nu mice, 6-8 weeks old)[1] | | Dosage: | 50 mg/kg; 100 mg/kg | | Administration: | Oral gavage; once daily; for 18 consecutive days | | Result: | Decreased the tumor volume and weight by 48% and 45%, respectively. |
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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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