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CAY10603

CAY10603

Catalog No.

B4856

HDAC6抑制剂

组合的产品项目
规格	价格	库存
10mM (in 1mL DMSO)	￥ 1,200.00	现货
1mg	￥ 600.00	现货
5mg	￥ 954.00	现货
25mg	￥ 3,090.00	现货

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背景
化学属性
试验操作
质量控制

背景

CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 2 pM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively)[1].

CAY10603 inhibits the proliferation and induces apoptosis of lung adenocarcinoma cells. In addition, CAY10603 works in concert with gefitinib to induce apoptosis in lung adenocarcinoma cell lines, in part due to EGFR instability and EGFR pathway inactivation[2].

In C57BL/6 mice model of endotoxemia, CAY10603 (intraperitoneal injection, 5 mg/kg, 2h) pretreatment significantly inhibits endotoxin-induced caspase-3 activation and reduces endotoxin-induced pulmonary edema form[3].

References:

[1]. Kozikowski A P, Tapadar S, Luchini D N, et al. Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: A new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. Journal of Medicinal Chemistry, 2008, 51(15): 4370-4373.

[2]. Wang Z, et al. HDAC6 promotes cell proliferation and confers resistance to gefitinib in lung adenocarcinoma. Oncol Rep, 2016, 36(1): 589-97.

[3]. Yu J, Ma M, Ma Z, et al. HDAC6 inhibition prevents TNF-α-induced caspase 3 activation in lung endothelial cell and maintains cell-cell junctions. Oncotarget, 2016, 7(34): 54714-54722.

化学属性

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	446.5
Cas No.	1045792-66-2
Formula	C₂₂H₃₀N₄O₆
Solubility	≥22.35 mg/mL in DMSO; insoluble in EtOH; ≥24.85 mg/mL in H2O
Chemical Name	tert-butyl N-[4-[3-[[7-(hydroxyamino)-7-oxoheptyl]carbamoyl]-1,2-oxazol-5-yl]phenyl]carbamate
SDF	Download SDF
Canonical SMILES	CC(C)(C)OC(=O)NC1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCCCCC(=O)NO
运输条件	蓝冰运输或根据您的需求运输。
一般建议	不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

试验操作

细胞实验 [1-4]:
细胞系	胰腺癌细胞系A549和H460细胞，非小细胞肺癌细胞
溶解方法	该化合物在DMSO中的溶解度大于22.4mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。
反应条件	0.1 μM，6 h
应用	CAY10603对胰腺癌细胞系有抗增殖活性，IC50小于1 μM。在Mia Paca-2和Panc04.03细胞中，CAY10603在100 nM浓度下具有活性，对HupT3细胞，在200-300 nM浓度下具有活性。CAY10603（0.1 μM，6h）阻断内皮细胞中TNF-α诱导的caspase-3活化。在HPAECs中，用CAY10603（0.1μM）预处理6小时抑制TNF-α诱导的内皮通透性。CAY10603（0.05 μM）显著降低NSCLC细胞的细胞活力。在A549和H460细胞中，CAY10603（0.01-0.16 μM）以剂量依赖性方式降低总EGFR表达和EGFR、AKT和ERK的磷酸化。在两种人肺腺癌细胞系A549和HCC827中，CAY10603 （0.02-0.32 μM）治疗以剂量依赖性方式降低细胞增殖。CAY10603减少了肺腺癌细胞系的克隆数。 CAY10603诱导肺腺癌A549细胞凋亡。CAY10603（0.01 μM）和吉非替尼（1 μM）组合给药48h，显著抑制A549细胞的克隆生存。
动物实验 [2]:
动物模型	内毒素血症C57BL/6小鼠模型
给药剂量	腹腔注射，5 mg/kg，2 h
应用	在内毒素血症的C57BL/6小鼠模型中，CAY10603预处理显著抑制内毒素诱导的caspase-3激活，减弱肺组织中内毒素诱导的肺水肿形成。
注意事项	由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。
References: [1]. Kozikowski, A. P., Tapadar, S., Luchini, D. N., Kim, K. H., & Billadeau, D. D. (2008). Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. Journal of medicinal chemistry, 51(15), 4370-4373. [2]. Yu, J., Ma, M., Ma, Z., & Fu, J. (2016). HDAC6 inhibition prevents TNF-α-induced caspase 3 activation in lung endothelial cell and maintains cell-cell junctions. Oncotarget, 7(34), 54714. [3]. Wang, Z., Hu, P., Tang, F., & Xie, C. (2016). HDAC6-mediated EGFR stabilization and activation restrict cell response to sorafenib in non-small cell lung cancer cells. Medical Oncology, 33(5), 50. [4]. Wang, Z., Tang, F., Hu, P., Wang, Y., Gong, J., Sun, S., & Xie, C. (2016). HDAC6 promotes cell proliferation and confers resistance to gefitinib in lung adenocarcinoma. Oncology reports, 36(1), 589-597.