BIX-01294 trihydrochloride
Based on 27 publication(s) in Google Scholar
BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 1392399-03-9
- Formula: C28H41Cl3N6O2
- Molecular Weight:600.02
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) BIX-01294 trihydrochloride
More- Nat Microbiol. 2025 Oct 10. [Abstract]
- ACS Nano. 2023 Feb 14;17(3):3181-3193. [Abstract]
- J Exp Clin Cancer Res. 2018 Aug 17;37(1):196. [Abstract]
- Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
- Cell Death Dis. 2019 Apr 15;10(5):331. [Abstract]
- Cell Death Dis. 2017 Apr 6;8(4):e2726. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- NPJ Regen Med. 2024 Apr 29;9(1):17. [Abstract]
- Biomolecules. 2026 Feb 25;16(3):345. [Abstract]
- Molecules. 2025 Jul 22;30(15):3054. [Abstract]
- Mol Med Rep. 2023 Feb;27(2):21. [Abstract]
- Mol Med Rep. 2021 Aug;24(2):616. [Abstract]
- J Cell Mol Med. 2022 Nov;26(21):5539-5550. [Abstract]
- iScience. 2021 Oct 14;24(11):103271. [Abstract]
- Biomedicines. 2020 Nov 9;8(11):485. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2018 May;1864(5 Pt A):1744-1753. [Abstract]
- Exp Cell Res. 2020 Aug 15;393(2):112090. [Abstract]
- Invest New Drugs. 2021 Jun;39(3):686-696. [Abstract]
- PLoS One. 2023 Aug 29;18(8):e0289510. [Abstract]
- Biochem Biophys Res Commun. 2026 Jan 1:794:153072. [Abstract]
- Biochem Biophys Res Commun. 2025 Jan:743:151171. [Abstract]
- Cell J. 2023 Feb 1;25(2):118-125. [Abstract]
- bioRxiv. 2024 Oct 30:2024.09.30.615828. [Abstract]
- Research Square Print. September 20th, 2022.
- Aging (Albany NY). 2021 Mar 19;13(7):9704-9718. [Abstract]
- bioRxiv. 2020 Jun.
- Patent. US20180263995A1.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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ELISA
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RT-PCR
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WB
All Histone Methyltransferase Isoforms
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Biological Activity
IC50: 2.7 μM (G9a in DELFIA assay)[2]
IC50: 1.9 μM for G9a and 0.7 μM for GLP[5]
BIX-01294 (2 μM; 48 h) trihydrochloride selectively inhibits recurrent tumor cell growth[1].
BIX-01294 (1 μM) trihydrochloride leads to a marked increase in phosphorylation of S345 of MLKL[1].
BIX-01294 (1 μM) trihydrochloride significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines[1].
BIX-01294 (1 μM; 6 days) trihydrochloride causes the reduction in H3K9me2 levels in primary and recurrent tumor cells[1].
BIX-01294 trihydrochloride leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h) trihydrochloride[1].
BIX-01294 (4.1 μM; for 2 days) trihydrochloride causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 trihydrochloride causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells[2].
BIX-01294 trihydrochloride has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 trihydrochloride does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)[2].
BIX-01294 trihydrochloride inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM)[2].
BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary or recurrent tumor cells
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Concentration:2 μM
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Incubation Time:48 h
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Result:Selectively inhibited recurrent tumor cell growth.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells[1]
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Dosage:10 mg/kg
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Administration:IP; three times a week for 2 weeks
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Result:Significantly reduced tumor growth and tumor burden in recurrent tumor cells.
Primary tumor growth was not inhibited.
Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.
Chemical Information
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CAS No. 1392399-03-9
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Appearance Solid
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Molecular Weight 600.02
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Formula C28H41Cl3N6O2
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Color Light yellow to yellow
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SMILES
CN(CCC1)CCN1C2=NC(C=C(OC)C(OC)=C3)=C3C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (27)
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Journal Impact Factor
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Most Recent
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Nat Microbiol
2025 Oct 10. PMID: 41073665
BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2025 Oct 10. [Abstract]
Both KL1 (40, 100 µM) and BIX-01294 (1, 4 µM) reduced ROS levels at 4 hpi. Chemiluminescent L-012 probes were used to quantify reactive species.
BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2025 Oct 10. [Abstract]
Inhibition of EHMT2/G9a phenocopied KL1-mediated sensitization in intracellular S. aureus. A selective EHMT2/G9a inhibitor, BIX-01294 (BIX; 1–10 µM), increased the bioluminescence signal (grey bars) of strain JE2-lux compared to the vehicle control (Veh; 0.1% DMSO). Cytotoxicity of BIX was also assessed (red circles). Representative data of 3 experiments (n = 6, two-sided unpaired t-test) were obtained.
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ACS Nano
Binary Colloidal Crystals Promote Cardiac Differentiation of Human Pluripotent Stem Cells via Nuclear Accumulation of SETDB1. [Abstract]2023 Feb 14;17(3):3181-3193. PMID: 36655945 -
J Exp Clin Cancer Res
2018 Aug 17;37(1):196. PMID: 30119635
BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 17;37(1):196. [Abstract]
The relative mRNA levels of Ki67 and PCNA in primary CRC cells responding to rhIL-33 (100 ng/mL) incubation and/ or indicated inhibitors (SB203580, 10 μg/mL; PD98059, 20 μg/mL; SP600125, 10 μg/mL; BIX01294, 2 μM; 5Aza, 10 μM; SC560, 0.1 μg/mL; celecoxib, 20 μg/mL) for 24 h.
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Adv Sci (Weinh)
KDM3A Ablation Activates Endogenous Retrovirus Expression to Stimulate Antitumor Immunity in Gastric Cancer. [Abstract]2024 Oct;11(40):e2309983. PMID: 39031630 -
Cell Death Dis
Ferritinophagy is required for the induction of ferroptosis by the bromodomain protein BRD4 inhibitor (+)-JQ1 in cancer cells. [Abstract]2019 Apr 15;10(5):331. PMID: 30988278 -
Cell Death Dis
G9A promotes tumor cell growth and invasion by silencing CASP1 in non-small-cell lung cancer cells. [Abstract]2017 Apr 6;8(4):e2726. PMID: 28383547
BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Apr 6;8(4):e2726. [Abstract]
Upper and middle panels: WB detection of H3K9me2 and G9A in PC9 and A549 cells treated with 0, 1, 2.5, 5 or 10 μM BIX-01294. The total level of histone H3 and actin serve as loading controls. Lower panel: WB detection of the total (T-) level of and phosphorylated (P-) ERK kinase in PC9 and A549 cells treated with 0, 1, 5 or 10 μM BIX-01294. GAPDH serves as the loading control
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Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
NPJ Regen Med
Epigenetic mechanisms regulate sex differences in cardiac reparative functions of bone marrow progenitor cells. [Abstract]2024 Apr 29;9(1):17. PMID: 38684697
BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: NPJ Regen Med. 2024 Apr 29;9(1):17. [Abstract]
CCL3 was found to be the most altered cytokine by inhibiting G9a using BIX-01294 (1 μM). Inhibition of G9a using BIX-01294 (1 μM) largely altered the secretion in the F-EPC and OVX-EPC. ELISA showed secretory upregulation of CCL3 and VEGF-A in M-EPC, F-EPC, and OVX-EPC with the inhibition of G9a using BIX-01294.
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Biomolecules
Targeting G9a Exerts Pleiotropic Suppression in Triple-Negative Breast Cancer Cells: Cooperatively Inducing Pyroptosis and Apoptosis. [Abstract]2026 Feb 25;16(3):345. PMID: 41897283 -
Molecules
Modulatory Effect of Curcumin on Expression of Methyltransferase/Demethylase in Colon Cancer Cells: Impact on wt p53, mutp53 and c-Myc. [Abstract]2025 Jul 22;30(15):3054. PMID: 40807229 -
Mol Med Rep
G9a inhibition promotes the formation of pacemaker-like cells by reducing the enrichment of H3K9me2 in the HCN4 promoter region. [Abstract]2023 Feb;27(2):21. PMID: 36484369 -
Mol Med Rep
H3K9me2 regulates early transcription factors to promote mesenchymal stem‑cell differentiation into cardiomyocytes. [Abstract]2021 Aug;24(2):616. PMID: 34184085 -
J Cell Mol Med
Larotrectinib induces autophagic cell death through AMPK/mTOR signalling in colon cancer. [Abstract]2022 Nov;26(21):5539-5550. PMID: 36251949 -
iScience
miR-1307 promotes hepatocarcinogenesis by CALR-OSTC-endoplasmic reticulum protein folding pathway. [Abstract]2021 Oct 14;24(11):103271. PMID: 34761190 -
Biomedicines
Exosome-Mediated Differentiation of Mouse Embryonic Fibroblasts and Exocrine Cells into β-Like Cells and the Identification of Key miRNAs for Differentiation. [Abstract]2020 Nov 9;8(11):485. PMID: 33182285 -
Biochim Biophys Acta Mol Basis Dis
2018 May;1864(5 Pt A):1744-1753. PMID: 29499325 -
Exp Cell Res
Lamin B2 promotes the malignant phenotype of non-small cell lung cancer cells by upregulating dimethylation of histone 3 lysine 9. [Abstract]2020 Aug 15;393(2):112090. PMID: 32416090 -
Invest New Drugs
BIX-01294, a G9a inhibitor, suppresses cell proliferation by inhibiting autophagic flux in nasopharyngeal carcinoma cells. [Abstract]2021 Jun;39(3):686-696. PMID: 33387131 -
PLoS One
DNA methylation cooperates with H3K9me2 at HCN4 promoter to regulate the differentiation of bone marrow mesenchymal stem cells into pacemaker-like cells. [Abstract]2023 Aug 29;18(8):e0289510. PMID: 37643180 -
Biochem Biophys Res Commun
Inhibition of histone-lysine N-methyltransferase G9a exacerbates alcoholic steatohepatitis (ASH) in mice. [Abstract]2026 Jan 1:794:153072. PMID: 41344213 -
Biochem Biophys Res Commun
Inhibition of histone methyltransferase G9a aggravates phenotypic severity of hepatic lipotoxicity in non-alcoholic steatohepatitis (NASH). [Abstract]2025 Jan:743:151171. PMID: 39693938 -
Cell J
2023 Feb 1;25(2):118-125. PMID: 36840458 -
bioRxiv
A host-directed adjuvant resuscitates and sensitizes intracellular bacterial persisters to antibiotics. [Abstract]2024 Oct 30:2024.09.30.615828. PMID: 39554024 -
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Aging (Albany NY)
Uhrf1 regulates H3K9me2 modification of mTOR to inhibit the effect of autophagy in myocardial ischemia-reperfusion injury. [Abstract]2021 Mar 19;13(7):9704-9718. PMID: 33744855 -
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Solvent & Solubility
H2O : ≥ 100 mg/mL (166.66 mM)
DMSO : 58.33 mg/mL (97.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nathaniel W Mabe, et al. G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep. 2020 Nov 3;33(5):108341. [Content Brief]
[2]. Stefan Kubicek, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81. [Content Brief]
[3]. Yang Q, et al. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012 Aug;45(4):335-44. [Content Brief]
[4]. Iwona Anna Ciechomska, et al. BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep [Content Brief]
[5]. Yanqi Chang, et al.Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol. 2009 Mar;16(3):312-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.6666 mL | 8.3331 mL | 16.6661 mL | 41.6653 mL |
| 5 mM | 0.3333 mL | 1.6666 mL | 3.3332 mL | 8.3331 mL | |
| 10 mM | 0.1667 mL | 0.8333 mL | 1.6666 mL | 4.1665 mL | |
| 15 mM | 0.1111 mL | 0.5555 mL | 1.1111 mL | 2.7777 mL | |
| 20 mM | 0.0833 mL | 0.4167 mL | 0.8333 mL | 2.0833 mL | |
| 25 mM | 0.0667 mL | 0.3333 mL | 0.6666 mL | 1.6666 mL | |
| 30 mM | 0.0556 mL | 0.2778 mL | 0.5555 mL | 1.3888 mL | |
| 40 mM | 0.0417 mL | 0.2083 mL | 0.4167 mL | 1.0416 mL | |
| 50 mM | 0.0333 mL | 0.1667 mL | 0.3333 mL | 0.8333 mL | |
| 60 mM | 0.0278 mL | 0.1389 mL | 0.2778 mL | 0.6944 mL | |
| 80 mM | 0.0208 mL | 0.1042 mL | 0.2083 mL | 0.5208 mL | |
| H2O | 100 mM | 0.0167 mL | 0.0833 mL | 0.1667 mL | 0.4167 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
BIX-01294 trihydrochloride Related Classifications
HY-108239 Related Classifications
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