TW-37
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.
TW-37是一种有效的BCL-2小分子抑制剂,Ki值为290 nmol/L,衰减BCL-2的活化,抑制多个BCL-2家族成员,包括BCL-XL(Ki = 1,110 nmol/L)和MCL-1(Ki = 260 nmol/L)。TW-37与BCL-2同源结构域3(BH 3)的沟结合,阻止促凋亡蛋白(比如Bid、Bim和Bad)与BCL-2的异二聚化,从而使它们诱导细胞凋亡。最近的研究表明,TW-37能够抑制一系列癌细胞(如乳腺癌、前列腺癌、淋巴瘤和胰腺癌)的生长,TW-37诱导S期细胞周期停滞,调控多个重要的细胞周期相关基因,包括p27、p57、E2F-1、cdc25A、CDK4、cyclin A、cyclin D1和cyclin E。
参考文献:
Zhiwei Wang, Asfar Sohail Azmi, Aamir Ahmad, Sanjeev Banerjee, Shaomeng Wang, Fazlul H. Sarkar, and Ramzi M. Mohammad. TW-37, a small-molecule inhibitor of BCL-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer Res 2009;69:2757-2765
Naoki Ashimori, Benjamin D. Zeitlin, Zhaocheng Zhang, Kristy Warner, IIan M. Turkienicz, Aaron C. Spalding, Theodoros N. Teknos, Shaomeng Wang, and Jacques E. Nor. TW-37, a small-molecule inhibitor of BCL-2, mediates S-phase cell cycle arrest and suppresses head and neck tumor angiogenesis. Mol Cancer Ther 2009;8:893-903
- 1. In-Hyoung Yang, Seung-Hyun Hong, et al. "Cryptotanshinone chemosensitivity potentiation by TW-37 in human oral cancer cell lines by targeting STAT3–Mcl-1 signaling." Cancer Cell Int 2020 Aug 26;20:405. PMID:32863764
- 2. Chi-Hyun Ahn, Won Woo Lee, et al. "Antitumor effect of TW-37, a BH3 mimetic in human oral cancer." Laboratory Animal Research. 04 December 2019.
- 3. Villalobos-Ortiz M, Ryan J, et al. "BH3 profiling discriminates on-target small molecule BH3 mimetics from putative mimetics." Cell Death Differ. 2019 Jul 22. PMID:31332296
- 4. Yang IH, Ahn CH, et al. "Heme Oxygenase-1 is a Key Molecule Underlying Differential Response of TW-37-Induced Apoptosis in Human Mucoepidermoid Carcinoma Cells." Molecules. 2019 May 1;24(9). pii: E1700. PMID:31052354
- 5. Russo M, Milito A, et al. "CK2 and PI3K are direct molecular targets of quercetin in chronic lymphocytic leukaemia." Oncotarget. 2017 Jun 27;8(26):42571-42587. PMID:28489572
Storage | Store at -20°C |
M.Wt | 573.7 |
Cas No. | 877877-35-5 |
Formula | C33H35NO6S |
Synonyms | TW37,TW 37 |
Solubility | insoluble in H2O; ≥19.75 mg/mL in DMSO; ≥3.41 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide |
SDF | Download SDF |
Canonical SMILES | CC(C)C1=CC=CC=C1CC2=C(C(=C(C(=C2)C(=O)NC3=CC=C(C=C3)S(=O)(=O)C4=CC=CC=C4C(C)(C)C)O)O)O |
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] | |
细胞系 |
BxPC-3和Colo-357细胞 |
制备方法 |
该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
细胞生长抑制:750 nM,72小时;凋亡诱导:500 nM,48小时(通过膜联蛋白V测量) |
实验结果 |
通过克隆形成实验评估细胞活力。与对照相比,TW-37显著抑制BxPC-3和Colo-357细胞的集落形成。此外,TW-37以剂量和时间依赖性方式诱导凋亡。在Annexin V测定中,凋亡细胞的百分比从对照组的5%-6%增加至BxPC-3和Colo-357细胞系中的12%-14% |
动物实验: [1] | |
动物模型 |
携带Colo-357异种移植物的雌性ICR-SCID小鼠 |
给药剂量 |
静脉注射,20 mg/kg/d |
实验结果 |
TW-37显著抑制体内胰腺肿瘤生长。Western印迹分析显示,TW-37处理小鼠的肿瘤中,Notch-1的表达水平显著低于对照组小鼠。此外,在TW-37处理的肿瘤中,Jagged-1和Notch-1下游靶基因Hes-1的表达下调。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1] Wang Z, Azmi A S, Ahmad A, et al. TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer: involvement of Notch-1 signaling pathway. Cancer research, 2009, 69(7): 2757-2765. |
TW-37是一种新型的非肽类抑制剂,作用于重组的Bcl-2、Bcl-xL和Mcl-1,Ki值分别为0.29 μM、1.11 μM和0.26 μM。. | ||||||
靶点 | Bcl-2 | Bcl-xL | Mcl-1 | |||
IC50 | 0.29 μM (Ki) | 1.11 μM (Ki) | 0.26 μM (Ki) |
质量控制和MSDS
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