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MCE 國際站:Polθ/PARP-IN-1
產(chǎn)品活性:Polθ/PARP-IN-1 (compound 25d) 是一種有效的雙 DNA 聚合酶 θ (DNA polymerase theta (Polθ)) 和 PARP 抑制劑,IC50 值分別為 45.6、5.4 nM。Polθ/PARP-IN-1 顯示出抗增殖活性。Polθ/PARP-IN-1 誘導細胞凋亡 (apoptosis) 和細胞周期停滯在 G2/M 期,導致 DNA 損傷。Polθ/PARP-IN-1 顯示出抗腫瘤活性。
研究領(lǐng)域:Apoptosis | Cell Cycle/DNA Damage | Epigenetics
作用靶點:Apoptosis | DNA/RNA Synthesis | PARP
In Vitro: Polθ/PARP-IN-1 (compound 25d) (0-80 M; 3 days) shows antiproliferative activity with IC50s of 20.9, 2.7, 8.9, 2.9, 18.9, >80 M for HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells, respectively.
Polθ/PARP-IN-1 (compound 25d) (2 M; 3 days) induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage.
In Vivo: Polθ/PARP-IN-1 (20, 40 mg/kg; i.p.; daily for 21 consecutive days) inhibits tumor growth in MDA-MB-436 xenograft model.
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