BIX 01294
For research use only. Not for use in humans.
Catalog No.S8006
13 publications
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.
3 Customer Reviews
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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.
J Pineal Res, 2018, 65(2):e12497. BIX 01294 purchased from Selleck.
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(H) Fold change of miR-200c expression in MCF7 cells under leptin and S3I-201/BIX01294 treatment (n=3, asterisk indicates P<0.05). Error bars denote ±SD.
Cancer Res, 2015, 75(11):2375-86. . BIX 01294 purchased from Selleck.
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Cells were treated by BIX-01294 1.5 μM for 48 h and then Brdu incorporation assay was taken out (×100).
PLoS One, 2015, 10(9):e0138390. BIX 01294 purchased from Selleck.
Purity & Quality Control
Choose Selective Histone Methyltransferase Inhibitors
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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| Assay |
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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 |
| Smiles | Cl.Cl.Cl.COC1=CC2=NC(=NC(=C2C=C1OC)NC3CCN(CC3)CC4=CC=CC=C4)N5CCCN(C)CC5 |
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