耗材描述
Dot1L-IN-5
产品活性:Dot1L-IN-5 是一种有效的类端粒沉默干扰体 1 (DOT1L) 抑制剂,IC50 为 0.17 nM。
产品来源: https://www.medchemexpress.cn/dot1l-in-5.html
研究领域:Epigenetics
作用靶点:Histone Methyltransferase
In Vitro: Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM).
In Vivo: Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition.
While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1.
相关产品:Bioactive Compound Library Plus | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Reprogramming Compound Library | Anti-Blood Cancer Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Anti-Hematopathy Compound Library | Bioactive Compound Library Max | GSK126 | Pinometostat | Tazemetostat | GSK3326595 | 3-Deazaneplanocin A hydrochloride | GSK343 | GSK3368715 dihydrochloride | BIX-01294 | EPZ015666 | EZM0414 TFA | Chaetocin | EED226 | MS023 | UNC1999 | Onametostat | OICR-9429 | EZM 2302 | MRTX-1719 | UNC0642 | UNC0379 | SGC0946 | UNC0224 | GSK591 | Sinefungin | EPZ004777 | MS177 | UNC0638 | A-366 | TP-064 | NSC 663284
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