Ex-527: Difference between revisions
imported>Kevin |
imported>Kevin No edit summary |
||
| (2 intermediate revisions by the same user not shown) | |||
| Line 2: | Line 2: | ||
"EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive." | "EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive." | ||
**-Sigma Description | **-Sigma Description | ||
"Selective inhibitor of SIRT1 that does not inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members (IC50 values are 98, 19600, 48700, > 100000 and > 100000 nM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Enhances p53 acetylation in response to DNA damaging agents." | |||
**-Tocris description | |||
[[File:EX527.png|frame|right|Ex-527 structure, photo from Sigma-Aldrich]] | [[File:EX527.png|frame|right|Ex-527 structure, photo from Sigma-Aldrich]] | ||
| Line 7: | Line 10: | ||
==Genes Affected== | ==Genes Affected== | ||
*[http://www.xenbase.org/gene/showgene.do?method=display&geneId=989002 sirt1] | *[http://www.xenbase.org/gene/showgene.do?method=display&geneId=989002 sirt1] | ||
*[http://www.xenbase.org/gene/showgene.do?method=display&geneId=5929104 sirt6] | *[http://www.xenbase.org/gene/showgene.do?method=display&geneId=5929104 sirt6] | ||
==Suppliers== | ==Suppliers== | ||
| Line 23: | Line 22: | ||
==References== | ==References== | ||
*[https://pubchem.ncbi.nlm.nih.gov/compound/5113032 PubChem] | |||
*[http://www.xenbase.org/literature/article.do?method=display&articleId=49378 Ohata et al., 2014] | *[http://www.xenbase.org/literature/article.do?method=display&articleId=49378 Ohata et al., 2014] | ||
>Search for other articles using EX-527 with [http://www.xenbase.org/cgi-bin/textpresso/xenopus/search textpresso] | >Search for other articles using EX-527 with [http://www.xenbase.org/cgi-bin/textpresso/xenopus/search textpresso] | ||
*[[Small Molecules for Xenopus Research|Back To Small Molecules Home Page]] | |||
Latest revision as of 12:44, 2 June 2015
Description
"EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive."
- -Sigma Description
"Selective inhibitor of SIRT1 that does not inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members (IC50 values are 98, 19600, 48700, > 100000 and > 100000 nM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Enhances p53 acetylation in response to DNA damaging agents."
- -Tocris description
Genes Affected
Suppliers
Usage Notes
References
>Search for other articles using EX-527 with textpresso