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.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
WEHI-539 is a small-molecule inhibitor of BCLXLwith an IC50 value of 1.1 nM .
WEHI-539 was designed as a BCL-XLinhibitor with high affinity. It interacted the with the binding groove of BCL-XLwith a Kd value of 0.6 nM. In MEF cells lacking MCL-1, WEHI-539 induced apoptosis which was evidenced by the release of mitochondrial cytochrome cand caspase-3 processing. In BCL-XLoverexpressed MEF cells, WEHI-539 showed EC50 value of 0.48 μM. WEHI-539 also significantly induced apoptosis of the platelets purified from mice. Besides that, WEHI-539can not kill MEF cells lacking BAK because the cell death mediator BAK is regulated by BCL-XLand MCL-1. .
 Lessene G, Czabotar P E, Sleebs B E, et al. Structure-guided design of a selective BCL-XL inhibitor. Nature chemical biology, 2013, 9(6): 390-397.
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- 2. Soderquist RS, Crawford L, et al. "Systematic mapping of BCL-2 gene dependencies in cancer reveals molecular determinants of BH3 mimetic sensitivity." Nat Commun. 2018 Aug 29;9(1):3513. PMID:30158527
- 3. Wilson Xuan Mai."Comprehensive Characterization of the Apoptotic Machinery in Glioblastoma Identifies New Therapeutic Strategies." UNIVERSITY OF CALIFORNIA.2018-01-01.
- 4. Dai J, Luftig MA. "Intracellular BH3 Profiling Reveals Shifts in Antiapoptotic Dependency in Human B Cell Maturation and Mitogen-Stimulated Proliferation." J Immunol. 2018 Mar 1;200(5):1727-1736. PMID:29358277
- 5. Vuillier C, Lohard S, et al. "E2F1 interacts with BCL-xL and regulates its subcellular localization dynamics to trigger cell death." EMBO Rep. 2017 Dec 12. PMID:29233828
- 6. Mai WX, Gosa L, et al. "Cytoplasmic p53 couples oncogene-driven glucose metabolism to apoptosis and is a therapeutic target in glioblastoma." Nat Med. 2017 Nov;23(11):1342-1351. PMID:29035366
- 7. Park HA, Licznerski P, et al. "Inhibition of Bcl-xL prevents pro-death actions of ΔN-Bcl-xL at the mitochondrial inner membrane during glutamate excitotoxicity."Cell Death Differ. 2017 Nov;24(11):1963-1974. PMID:28777375
- 8. Tan Y, Lin Y, et al. "Selective Antagonism of Bcl-xL Potentiates M1 Oncolysis by Enhancing Mitochondrial Apoptosis." Hum Gene Ther. 2017 Jul 27. PMID:28750564
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|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||insoluble in DMSO,insoluble in EtOH,insoluble in H2O|
|Chemical Name||5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[(8E)-8-(1,3-benzothiazol-2-ylhydrazinylidene)-6,7-dihydro-5H-naphthalen-2-yl]-1,3-thiazole-4-carboxylic acid|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
Human colon cancer cell
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
1 μM, 24h
Limiting dilution analysis with CSCs that were pre-treated with ABT-737, ABT-199 or WEHI-539 revealed that ABT-737 and WEHI-539 both were sufficient to decrease clonogenic capacity, whereas ABT-199 did not affect clonogenic growth. As WEHI-539 is selective for BCLXL, this points to a dependency of CSCs on BCLXL for survival. Importantly, ABT-737- or WEHI-539-induced loss of clonogenicity could be restored when BCLXL was ectopically overexpressed. When spheroid cultures were treated with ABT-737 or WEHI-539 compounds, CSCs were effectively sensitized toward oxaliplatin and other chemotherapeutic agents.
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.
|WEHI-539, has high affinity (subnanomolar) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. WEHI-539 has a high affinity for BCL-XL (IC50 = 1.1 nM).|
Quality Control & MSDS
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