WEHI-539 hydrochloride
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.
WEHI-539 hydrochloride是BCLXL的小分子抑制剂,IC50值为1.1 nM [1]。
WEHI-539是一种高亲和性的BCLXL抑制剂,与BCL-XL的特定结构域相互作用,Kd值为0.6 nM。在缺乏MCL-1的MEF细胞中,WEHI-539诱导细胞凋亡,证据显示线粒体细胞色素C的释放和caspase-3的加工。在BCL-XL过表达的MEF细胞中,WEHI-539诱导细胞凋亡,EC50值为0.48 μM。
WEHI-539也可以显著诱导从小鼠中纯化的血小板细胞的凋亡。由于促凋亡调节蛋白BAK是由BCL-XL和MCL-1调控的,因此,WEHI-539不能诱导缺乏BAK的MEF细胞的凋亡[1]。
参考文献:
[1]. Lessene G, Czabotar PE, Sleebs BE, et al. Structure-guided design of a selective BCL-XL inhibitor. Nature chemical biology, 2013, 9(6): 390-397.
- 1. Kim YJ, Tsang T, et al. "Inhibition of BCL2 family members increases the efficacy of copper chelation in BRAFV600E-driven melanoma." Cancer Res. 2020;canres.1784.2019. PMID:32005716
- 2. Rose JC, Dieter EM, et al. "Examining RAS pathway rewiring with a chemically inducible activator of RAS." Small GTPases. 2018 Apr 10:1-8. PMID:29634387
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 620.18 |
Cas No. | 2070018-33-4 |
Formula | C31H30ClN5O3S2 |
Solubility | ≥28.55 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | (E)-5-(3-(4-(aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazono)-5,6,7,8-tetrahydronaphthalen-2-yl)thiazole-4-carboxylic acid |
SDF | Download SDF |
Canonical SMILES | O=C(C1=C(C([H])([H])C([H])([H])C([H])([H])OC2=C([H])C([H])=C(C([H])([H])N([H])[H])C([H])=C2[H])SC(C3=C([H])C4=C(C([H])=C3[H])C([H])([H])C([H])([H])C([H])([H])/C4=N\N([H])C5=NC6=C([H])C([H])=C([H])C([H])=C6S5)=N1)O[H] |
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 |
人结肠癌细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
1 μM,24h |
应用 |
ABT-737、ABT-199或WEHI-539预处理肿瘤干细胞(CSCs)的有限稀释分析表明,ABT-737 和WEHI-539可以有效降低克隆能力,而ABT-199不影响克隆的生长。由于WEHI-539对BCLXL的选择性,表明CSCs的存活依赖于BCLXL。当BCLXL异位过表达时,ABT-737或WEHI-539诱导的克隆形成损失可以恢复。当球体细胞培养物用ABT-737或WEHI-539处理后,CSCs对oxaliplatin和其它的化疗药物变得敏感。 |
References: 1. Colak S, Zimberlin CD, Fessler E et al. Decreased mitochondrial priming determines chemoresistance of colon cancer stem cells. Cell Death Differ. 2014 Jul;21(7):1170-7. |
质量控制和MSDS
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