| 产品描述: | 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 |
| 靶点: |
HBO1;Apoptosis; HistoneMethyltransferase; HistoneAcetyltransferase |
| 体外研究: |
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 Cell Viability Assay Cell Line: Primary human OS (pOS-1) cells Concentration: 1, 5, 10, 25 uM Incubation Time: 24, 48, 72, 96 hours Result: Inhibited pOS-1 cell viability in a concentration-dependent manner.Exerted a significant anti-survival activity at least 48 h, displaying a time-dependent manner. Apoptosis Analysis Cell Line: pOS-1 cells Concentration: 5 uM Incubation Time: 72 hours Result: Activated cell apoptosis and significantly increases TUNEL-positive nuclei. RT-PCR Cell Line: pOS-1 cells Concentration: 5 uM Incubation Time: 24 hours Result: Downregulated MYLK-HOXA9 mRNA expression. |
| 体内研究: |
WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice. Animal Model: SCID mice (18-19 g, female) with pOS1 cells Dosage: 10 mg/kg Administration: IP; daily; for 21 days Result: Potently inhibited pOS-1 xenograft growth. |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.497 ml |
12.487 ml |
24.974 ml |
| 5 mM |
0.499 ml |
2.497 ml |
4.995 ml |
| 10 mM |
0.25 ml |
1.249 ml |
2.497 ml |
| 50 mM |
0.05 ml |
0.25 ml |
0.499 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |