BIX-01294 hydrochloride hydrate
Based on 26 publication(s) in Google Scholar
BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.
For research use only. We do not sell to patients.
- CAS No.: 1808255-64-2
- Formula: C28H38N6O2.3ClH.xH2O
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) BIX-01294 hydrochloride hydrate
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]
- 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.
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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
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G9a 1.7 μM (IC50) |
GLP 38 μM (IC50) |
BIX-01294 hydrochloride hydrate (1-10 μM) induces autophagy and apoptosis and reduces cell viability in LN18 glioma cells[1]. BIX-01294 hydrochloride hydrate (1-10 μM) upregulates levels of autophagy-related genes LC3B, WIPI1 and downregulates the differentiation-related genes GFAP, TUBB3, results in an autophagy-dependent differentiation in glioma stem-like cells (GSC)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LN18
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Concentration:1–10 μM
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Incubation Time:24-72 h
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Result:Reduced cell viability of LN18 in a dose-dependent manner.
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Cell Line:LN18
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Concentration:1–10 μM
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Incubation Time:24-72 h
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Result:Increased levels of cleaved caspase3/7 and cleaved PARP. Decreased levels of H3K9me2, H3K27me3 and accumulation of LC3-II.
Chemical Information
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CAS No. 1808255-64-2
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Formula C28H38N6O2.3ClH.xH2O
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SMILES
COC1=CC2=C(NC3CCN(CC3)CC4=CC=CC=C4)N=C(N5CCN(CCC5)C)N=C2C=C1OC.Cl.O.Cl.Cl.[x]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (26)
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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 hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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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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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Purity & Documentation
References
[1]. Ciechomska IA, et al., BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep. 2016 Dec 9;6:38723. [Content Brief]
[2]. Kubicek S, O'Sullivan RJ, August EM, Hickey ER, Zhang Q, Teodoro ML, Rea S, Mechtler K, Kowalski JA, Homon CA, Kelly TA, Jenuwein T. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81. [Content Brief]
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