BIX 01294
Catalog No.S8006
Molecular Weight(MW): 600.02
BIX01294 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.
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Biological Activity
| Description | BIX01294 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. | ||||||||||||||||
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| Targets |
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| In vitro |
BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. [1] BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1. [2] |
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| Cell Data |
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Protocol
Solubility (25°C)
| In vitro | DMSO | 98 mg/mL (163.32 mM) |
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| Water | 98 mg/mL (163.32 mM) | |
| Ethanol | 8 mg/mL (13.33 mM) |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 600.02 |
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| Formula | C28H38N6O2.3HCl |
| CAS No. | 1392399-03-9 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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