WM-3835 是一种有效的,高特异性HBO1(KAT7orMYST2) 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。
生物活性 | WM-3835 is a potent and high-specificHBO1(KAT7orMYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activatesapoptosiswhile inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice[1]. |
体外研究 (In Vitro) | 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) downregulatesMYLK-HOXA9mRNA 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].
Cell Viability Assay[1] 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[1] Cell Line: | pOS-1 cells | Concentration: | 5 uM | Incubation Time: | 72 hours | Result: | Activated cell apoptosis and significantly increases TUNEL-positive nuclei. |
RT-PCR[1] Cell Line: | pOS-1 cells | Concentration: | 5 uM | Incubation Time: | 24 hours | Result: | DownregulatedMYLK-HOXA9mRNA expression. |
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体内研究 (In Vivo) | WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice[1].
Animal Model: | SCID mice (18-19 g, female) with pOS1 cells[1] | Dosage: | 10 mg/kg | Administration: | IP; daily; for 21 days | Result: | Potently inhibited pOS-1 xenograft growth. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : 250 mg/mL(624.34 mM;Need ultrasonic) 配制储备液 1 mM | 2.4974 mL | 12.4869 mL | 24.9738 mL | 5 mM | 0.4995 mL | 2.4974 mL | 4.9948 mL | 10 mM | 0.2497 mL | 1.2487 mL | 2.4974 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.19 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.19 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.19 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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