HA14-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
HA14-1是一个有效的B细胞淋巴瘤因子2(Bcl-2)的小分子抑制剂,可结合并使细胞凋亡蛋白前体(如Bax和唯BH3家族蛋白)失活。在NIH3T3、HL60和肺癌H1299细胞系中有效地抑制Bcl-2抗凋亡并诱导细胞凋亡,对三者的IC50值在10 - 20 μM之间。HA14-1模仿同类-和异质二聚体形成所需的BH3域结合Bcl-2,阻止其他蛋白的结合导致HA14-1对Bcl-2的抑制。HA14-1已被广泛地用于细胞凋亡的研究中,表明它可用于癌症的治疗。
参考文献:
[1]. Chen J, Freeman A, Liu J, Dai Q, Lee RM. The apoptotic effect of HA14-1, a Bcl-2-interacting small molecular compound, requires Bax translocation and is enhanced by PK11195. Mol Cancer Ther. 2002 Oct;1(12):961-7.
[2]. Niino S, Nakamura Y, Hirabayashi Y, Nagano-Ito M, Ichikawa S. A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase. Biochem Biophys Res Commun. 2013 Apr 5;433(2):170-4. doi: 10.1016/j.bbrc.2013.02.052. Epub 2013 Feb 26.
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 409.23 |
Cas No. | 65673-63-4 |
Formula | C17H17BrN2O5 |
Solubility | insoluble in H2O; ≥20.45 mg/mL in DMSO; ≥41.53 mg/mL in EtOH with ultrasonic |
Chemical Name | ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate |
SDF | Download SDF |
Canonical SMILES | CCOC(=O)C1=C(OC2=C(C1C(C#N)C(=O)OCC)C=C(C=C2)Br)N |
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。 |
细胞实验 [1-3]: | |
细胞系 |
HL-60细胞,滤泡淋巴瘤B细胞系,HF1A3,HF4.9和HF28RA细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于20.5 mg/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 |
50 μM,4 h |
应用 |
在HL-60细胞中,HA14-1以剂量依赖的方式诱导细胞死亡。HA14-1(50 μM)导致超过90%的细胞活力丧失。在HL-60细胞中,HA14-1(50μM)处理3小时诱导DNA断裂。在滤泡淋巴瘤B细胞系HF1A3、HF4.9和HF28RA细胞中,HA14-1降低细胞活力并诱导凋亡。HA14-1(10-20 μmol/L)增加人胶质母细胞瘤细胞对放疗诱导的凋亡和化疗诱导的细胞凋亡的敏感性。 |
动物实验 [3]: | |
动物模型 |
BeGBM细胞攻击的Swiss裸鼠 |
给药剂量 |
腹腔注射,400 nM,从第2天开始每周一次 |
应用 |
在用BeGBM细胞攻击的免疫缺陷Swiss裸鼠中,从第2天开始每周一次HA14-1(400 nmol)对胶质母细胞瘤肿瘤的生长没有显著影响。HA14-1(400 nM)增加了DNA损伤剂etoposide (2.5 mg/kg)对体内胶质母细胞瘤生长的影响。 |
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]. Wang J L, Liu D, Zhang Z J, et al. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells[J]. Proceedings of the National Academy of Sciences, 2000, 97(13): 7124-7129. [2]. Skommer J, Wlodkowic D, Mtt M, et al. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells[J]. Leukemia research, 2006, 30(3): 322-331. [3]. Manero F, Gautier F, Gallenne T, et al. The small organic compound HA14-1 prevents Bcl-2 interaction with Bax to sensitize malignant glioma cells to induction of cell death[J]. Cancer research, 2006, 66(5): 2757-2764. |
HA14-1是Bcl-2表面口袋的非肽配体,IC50值9 μM。M | ||||||
靶点 | Bcl-2 | |||||
IC50 | 9 μM |
质量控制和MSDS
- 批次: