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CAS No. : 2413587-26-3
MCE 国际站:Tubulin/HDAC-IN-1
产品活性:Tubulin/HDAC-IN-1 是一种双重的 tubulin 和 HDAC-IN-1 抑制剂,其通过与 tubulin 的 CH/π 相互作用以及与 HDAC8 的氢键相互作用而发挥功能。Tubulin/HDAC-IN-1 可抑制 tubulin 聚合并选择性抑制 HDAC8 (IC50: 150 nM)。Tubulin/HDAC-IN-1 对各种人类癌细胞具有细胞毒性,还可将细胞周期阻滞在 G2/M 期并诱导细胞凋亡 (apoptosis)。Tubulin/HDAC-IN-1 可用于神经母细胞瘤、白血病等血液肿瘤和实体肿瘤的研究。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton | Epigenetics | Apoptosis | Metabolic Enzyme/Protease
作用靶点:Microtubule/Tubulin | HDAC | Apoptosis | Mitochondrial Metabolism
In Vitro: Tubulin/HDAC-IN-1 (Compound 12a, 72 h) shows cytotoxicity against various human cancer cell lines with an averaged IC50 value of 0.6 nM.
Tubulin/HDAC-IN-1 (2 nM, 24 h) induces HT29 cell cycle arrest in the G2/M phase and produces caspase-induced apoptosis of HT29 cells through mitochondrial dysfunction.
Tubulin/HDAC-IN-1 selectively inhibits HDAC8 (IC50: 150 nM), inhibits HDAC6 and HDAC11 with IC 50 values of 1 μM and 1.9 μM respectively.
Tubulin/HDAC-IN-1 (0.5-100 nM, 24 h/30 min) dose-dependently increases γH2AX level and acetylated SMC3 in HT-29 cells.
Tubulin/HDAC-IN-1 (5-15 μΜ, 0-40 min) inhibits tubulin polymerization in a dose-dependent manner, with a maximal effect achieved at 10 μM.
Tubulin/HDAC-IN-1 (250 nM, 30 min) depolymerizes the cell microtubule network, and the effect is not specific.
Tubulin/HDAC-IN-1 shows good in vitro metabolic stability expressed by the intrinsic clearance CLint (given in μL/min/mg protein) using rat liver microsomes (RLM) and human liver microsomes (HLM).
Compound |
RLM |
RLM |
HLM |
HLM |
|
t1/2 (h) |
CLint |
t1/2 |
CLint |
Tubulin/HDAC-IN-1 |
6.6 |
1.75 |
32 |
0.36 |
In Vivo: Tubulin/HDAC-IN-1 (Compound 12a, intratumoral injection, 0.25 mg/kg, three times a week for two weeks) decreases MCA205 tumor growth and extends the overall survival of treated mice in allogeneic sarcoma mice model.
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