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.
Because of the high levels of plasma-protein binding exhibited by WM-8014, WM-8014 can’t be used in vivo in mice. Development of derivatives of WM-8014 resulted in WM-1119, which has reduced plasma-protein binding. The interaction of WM-1119 with KAT6A is similar to that of WM-8014.
WM-1119 is also a highly potent, selective, reversible, and competitive inhibitor for KAT6A and KAT6B (histone lysine acetyltransferases). KD value of WM-1119 is 2 nM, compared to 5 nM for WM-8014.It is also competitive with acetyl-CoA, and driven by fast association kinetics. The structure of MYSTCryst in complex with WM-1119 was found to be almost identical to that of MYSTCryst–WM-8014.
WM-1119 induce cell cycle exit and cellular senescence without causing DNA damage. Senescence is INK4A/ARF-dependent and is accompanied by changes in gene expression that are typical of loss of KAT6A function. WM-1119, which has increased bioavailability, arrests the progression of lymphoma in mice. Notably, the activity of WM-1119 in this cell-based assay is an order of magnitude greater than WM-8014 and WM-1119 is able to induce cell cycle arrest at 1 μM. WM-1119 (IC50 0.25 μM) was ninefold more active than WM-8014 (IC50 2.3 μM), as expected on the basis of reduced protein binding.
WM-1119 is rapidly cleared after intraperitoneal injection, with the plasma concentration decreasing to below 1 μM after 4–6 h. By day 14, the cohorts that were treated four times per day with WM-1119 had arrested tumour growth. Spleen weights in the WM-1119-treatment group (treated four times per day) were substantially lower than spleen weights in the vehicle-treated group, and not significantly different from those of tumour-free eight-weekold mice.
. Baell JB1,2, Leaver DJ3，et, al, Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1.
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|