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.
Ki: 6 nM for BCL-2 TR-FRET
A-1331852 is a potent and selective inhibitor of BCL-XL.
Apoptosis is reported to be regulated by a family of closely related proteins exemplified by B cell lymphoma protein 2 (BCL-2), which is the first discovered family member. BCL-2 family proteins are divided by one to four BCL-2 homology motifs and can be further subdivided into pro- and antiapoptotic subsets.
In vitro: A-1331852 was identified as a potent BCL-XL inhibitor demonstrating cellular activity 10- to 50-fold more potent than its analog A-1155463 and the previouly reported BCL-XL inhibitor, navitoclax, respectively. Moreover, A-1331852 could selectively disrupt BCL-XL–BIM complexes and induce the apoptosis hallmarks in BCL-XL–dependent Molt-4 cells with median IC50 values in the low nanomolar range but did not affect MEF cells without BAK or BAX .
In vivo: Previous animal study found that A-1331852 could demonstrate antitumor efficacy in the Molt-4 xenograft model, such as tumor regressions as a single agent. In addition, in the NCI-H1963.FP5 xenograft model of SCLC, it was found that A-1331852 combined with venetoclax was able to recapitulate the efficacy of navitoclax .
Clinical trial: Up to now, A-1331852 is still in the preclinical development stage.
 Leverson JD et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642.
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Chemical Name||3-(1-(adamantan-1-ylmethyl)-5-methyl-1H-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)picolinic 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.|