WM-3835 是一种有效的，高特异性 HBO1 (KAT7 or MYST2) 抑制剂，可直接与 HBO1 33 的乙酰辅酶 A 结合位点结合 WM-3835 激活细胞凋亡，同时抑制骨肉瘤 (OS) 细胞的增殖，迁移和侵袭。WM-3835 具有抗肿瘤活性，并有效抑制小鼠中骨肉瘤异种移植物的生长。
货号:ajcx33060
CAS:2229025-70-9
分子式:C20H17FN2O4S
分子量：400.42
溶解度:DMSO : 250 mg/mL (624.34 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice[1].

WM-3835 (1-25 uM; 24-96 hours) inhibits pOS-1 cell viability in a concentration-dependent manner[1]. WM-3835 (5 uM; 72 h) activates cell apoptosis and significantly increases TUNEL-positive nuclei in pOS-1 cells[1]. WM-3835 (5 µM; 24 hours) downregulates MYLK-HOXA9 mRNA expression in pOS-1 cells[1]. WM-3835 (1-25 uM) suppresses H4K12ac-H3K14ac in a dose-dependent manner. WM-3835 does not alter the expressions of HBO1 protein and total H3, H4 histones[1]. WM-3835 (5 µM) fails to induce apoptosis and reduction of viability in HBO1-KO pOS-1 cells, koHBO1-1 and koHBO1-2, HBO1-low human osteoblasts[1].

WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice[1].

[1]. Yan-Yang Gao, et al. The histone acetyltransferase HBO1 functions as a novel oncogenic gene in osteosarcoma. Theranostics. 2021 Mar 4;11(10):4599-4615.