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。

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.

Solid

WM-3835 (1-25 uM; 24-96 hours) inhibits pOS-1 cell viability in a concentration-dependent manner.
WM-3835 (5 uM; 72 h) activates cell apoptosis and significantly increases TUNEL-positive nuclei in pOS-1 cells.
WM-3835 (5 μM; 24 hours) downregulates MYLK-HOXA9 mRNA expression in pOS-1 cells.
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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice (18-19 g, female) with pOS

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[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.

In Vitro: DMSO : 250 mg/mL (624.34 mM; Need ultrasonic)配制储备液