G9a/GLP
Inhibitory Selectivity
Isoform-specific Inhibitors
G9a/GLP Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8006 |
BIX 01294BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3. |
The H3K9me2 inhibitor BIX01294 mimics the effects of BPA and DEHP on the expression of meiotic genes and Plzf in cultured testes. (A) representative double IF staining for Mvh (green) and Stra8 (red) and Scp3 (red) and (B) Plzf (red) in histological sections of control and BIX01294-treated testes. (C) RT-qPCR analysis of Stra8, Scp3, Rec8, Spo11 and plzf in testes from the control and BIX01294-treated groups. Data are represented as the mean ± SEM. ns, P > 0.05, *P < 0.05; **P < 0.01.
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| S8071 |
UNC0638UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities. |
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| S7230 |
UNC0642UNC0642 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. |
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| S8068 |
ChaetocinChaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR). |
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| S7572 |
A-366A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. |
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| S7591 |
BRD4770BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8006 |
BIX 01294BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3. |
The H3K9me2 inhibitor BIX01294 mimics the effects of BPA and DEHP on the expression of meiotic genes and Plzf in cultured testes. (A) representative double IF staining for Mvh (green) and Stra8 (red) and Scp3 (red) and (B) Plzf (red) in histological sections of control and BIX01294-treated testes. (C) RT-qPCR analysis of Stra8, Scp3, Rec8, Spo11 and plzf in testes from the control and BIX01294-treated groups. Data are represented as the mean ± SEM. ns, P > 0.05, *P < 0.05; **P < 0.01.
|
|
| S8071 |
UNC0638UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities. |
||
| S7230 |
UNC0642UNC0642 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. |
||
| S8068 |
ChaetocinChaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR). |
||
| S7572 |
A-366A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. |
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| S7591 |
BRD4770BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence. |
