XY1 is a close analogue of SGC707, is completely inactive againstPRMT3 at concentrations as high as 100 μM. XY1 contains a naphthyl group replacing the isoquinoline group, lacks the key hydrogen bond with T466. The naphthyl ring of XY1 could act as a weak hydrogen-bond acceptor, but this should come with a substantial enthalpic penalty. The more than 1000-fold potency loss of XY1 compared with SGC707 supports this analysis. It is unclear whether other factors such as electronic effects also contributed to the potency loss of XY1 compared with SGC707. SGC707 and XY1 are a pair of excellent tools for the biomedical community to further elucidate biological functions and disease associations of PRMT3.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
MART-1- and gp100-expressing and -non-expressing melanoma cells are equally proliferative in tumors and clonogenic in vitro.
Aris M, et al. J Invest Dermatol. 2012 Feb;132(2):365-74. PMID: 21993558.
Change in the ileal bacterial population of turkeys fed different diets and after infection with Salmonella as determined with denaturing gradient gel electrophoresis of amplified 16s ribosomal DNA.
Santos AA Jr, et al. Poult Sci. 2008 Jul;87(7):1415-27. PMID: 18577625.
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EPZ011989 is a potent, orally-available EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646.
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UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.
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