UNC0638 hydrate
Based on 12 publication(s) in Google Scholar
UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets.
For research use only. We do not sell to patients.
- CAS No.: 1255517-77-1
- Formula: C30H49N5O3
- Molecular Weight:527.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) UNC0638 hydrate
More- Cancer Res. 2026 Jun 10. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
- Acta Pharmacol Sin. 2025 Aug 19. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- Cell Chem Biol. 2022 Jul 21;29(7):1153-1161.e5. [Abstract]
- Cell Biosci. 2023 Jan 12;13(1):7. [Abstract]
- Mol Med Rep. 2018 Feb;17(2):2239-2244. [Abstract]
- J Neurosci. 2025 Feb 5;45(6):e1790242024. [Abstract]
- Mol Carcinog. 2024 Nov;63(11):2119-2132. [Abstract]
- bioRxiv. 2023 Nov 17.
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WB
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
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RT-PCR
All Histone Methyltransferase Isoforms
More
Biological Activity
Description
IC50 & Target
IC50: <15 nM (G9a), 19±1 nM (GLP)[1]
Chemical Information
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CAS No. 1255517-77-1
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Molecular Weight 527.74
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Formula C30H49N5O3
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SMILES
CC(N1CCC(NC2=C3C=C(OC)C(OCCCN4CCCC4)=CC3=NC(C5CCCCC5)=N2)CC1)C.O
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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 (12)
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Journal Impact Factor
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Most Recent
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Cancer Res
TNG917 is a Potent and Selective Inhibitor of Histone Lysine Methyltransferases EHMT1/2 that Enhances Anti-Tumor Immunity and Immunotherapy Efficacy. [Abstract]2026 Jun 10. PMID: 42268285 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Death Dis
Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. [Abstract]2018 Jan 26;9(2):129. PMID: 29374157
UNC0638 hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
The effects of treatment with UNC0638 (10 μM) on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.
UNC0638 hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
The EHMT2 inhibitor UNC0638 (5-10 μM; 48 h) effectively inhibited cell growth in both PC9/ER and HCC827/ER cells.
UNC0638 hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
UNC0638 (100 nM; 48 h) suppressed cell migration in PC9 and PC9/ER cells.
UNC0638 hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
UNC0638 (100 nM; 48 h) pretreatment enhanced the sensitivity of PC9/ER cells to Erlotinib compared to non-pretreated cells.
UNC0638 hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
Treatment with UNC0638 (10 μM) resulted in the downregulation of Bcl-2 and VEGF in EGFR-TKI-resistant NSCLC cell lines.
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Acta Pharmacol Sin
DNMT inhibition epigenetically restores the cGAS-STING pathway and activates RIG-I/MDA5-MAVS to enhance antitumor immunity. [Abstract]2025 Aug 19. PMID: 40830678 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Cell Chem Biol
Visualization of the dynamic interaction between nucleosomal histone H3K9 tri-methylation and HP1α chromodomain in living cells. [Abstract]2022 Jul 21;29(7):1153-1161.e5. PMID: 35728598 -
Cell Biosci
Activation of goblet cell Piezo1 alleviates mucus barrier damage in mice exposed to WAS by inhibiting H3K9me3 modification. [Abstract]2023 Jan 12;13(1):7. PMID: 36631841 -
Mol Med Rep
UNC0638, a G9a inhibitor, suppresses epithelial‑mesenchymal transition‑mediated cellular migration and invasion in triple negative breast cancer. [Abstract]2018 Feb;17(2):2239-2244. PMID: 29207160
UNC0638 hydrate purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2018 Feb;17(2):2239-2244. [Abstract]
UNC0638 (0.5 and 1 µM; 24 h) suppressed triple negative breast cancer cell migration and invasion by regulating EMT-associated proteins. Western blots of EMT-associated proteins were performed.
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J Neurosci
Histone Methyltransferase G9a in Primary Sensory Neurons Promotes Inflammatory Pain and Transcription of Trpa1 and Trpv1 via Bivalent Histone Modifications. [Abstract]2025 Feb 5;45(6):e1790242024. PMID: 39824634 -
Mol Carcinog
A novel high-risk model identified by epithelial-mesenchymal transition predicts prognosis and radioresistance in rectal cancer. [Abstract]2024 Nov;63(11):2119-2132. PMID: 39056517 -
Protocols
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Spheroid/Tumor Organoid Invasion Assay
The spheroid/tumor organoid invasion assay measures outward movement of cancer cells from a compact 3D aggregate into an extracellular matrix, usually collagen I, basement membrane matrix, or mixed collagen-Matrigel hydrogels; the readout is generated by bright-field, fluorescence, confocal, or time-lapse imaging of cell egress, invasion area, invasion distance, dispersion, protrusion formation, basement-membrane perforation, or cell trajectories. The assay reflects cell-cell cohesion, cell-matrix adhesion, matrix remodeling, protease-dependent invasion, contractility, and invasion behavior in a 3D microenvironment rather than migration on a flat 2D surface.
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Ex Vivo Tissue Slice/Explant Invasion Assay
Ex vivo organotypic tissue slice cultures are based on maintaining thin, viable tissue sections at an air-liquid interface to preserve native cytoarchitecture and local cell-matrix interactions, enabling observation of cell behavior such as migration and tissue infiltration within a physiologically relevant 3D microenvironment. The method relies on maintaining tissue viability on porous membrane supports, allowing diffusion of nutrients and oxygen while preserving structural integrity for extended culture periods, which makes it suitable for studying dynamic cellular processes in intact tissue contexts such as cell movement and tissue remodeling. .
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Patient-Derived Organoid Invasion Assay
Patient-derived organoid (PDO) invasion assays are based on the ability of epithelial tumor organoids to self-organize in three-dimensional extracellular matrix (ECM) hydrogels (commonly Matrigel) and to recapitulate key aspects of in vivo tissue architecture, including polarity, proliferation, and invasive outgrowth when exposed to permissive microenvironmental cues. In this system, invasion is operationally defined as the emergence of multicellular protrusions, collective budding, or single-cell dissemination from the organoid core into the surrounding ECM, reflecting epithelial-mesenchymal plasticity and matrix remodeling capacity. Organoid morphology and invasive behavior are typically monitored using brightfield or confocal microscopy over time, enabling quantitative assessment of invasion area, protrusion number, and structural disruption of the organoid spheroid architecture.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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3D Tumor Spheroid Invasion Assay
3D tumor spheroid invasion assay measures outward tumor-cell movement from a compact multicellular spheroid into a surrounding extracellular matrix, producing image-based readouts such as invasion area, invasion distance, cell dispersion, or time-resolved cell movement. The method models tumor-cell interaction with matrix components in three dimensions and is used to study invasive phenotypes in cancer models including glioblastoma, squamous cell carcinoma, breast cancer, prostate cancer, ovarian cancer, and other solid tumor systems.
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Matrigel Transwell/Boyden Chamber Invasion Assay
Matrigel Transwell/Boyden chamber invasion assay measures the ability of cells to degrade or traverse an extracellular matrix-coated porous membrane and move from an upper chamber toward a chemoattractant in a lower chamber. Invasion is distinguished from migration by coating the membrane with Matrigel or basement membrane matrix; uncoated inserts measure migration, while coated inserts require cells to cross an ECM barrier before reaching the underside of the membrane.
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Invadopodia/Fluorescent Gelatin Degradation Assay
Invadopodia/fluorescent gelatin degradation assay detects proteolytic extracellular matrix degradation by cancer-cell invadopodia, which are actin-rich protrusive structures associated with matrix remodeling, invasion, and metastasis. The readout is generated by culturing cells on fluorescent gelatin and measuring dark degraded areas where fluorescent substrate has been locally removed, often together with immunofluorescent detection of invadopodia markers such as F-actin, cortactin, and TKS5.
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Organotypic 3D Invasion Assay
The organotypic 3D invasion assay measures carcinoma-cell invasion into a fibroblast-remodeled extracellular matrix, usually collagen I with or without basement-membrane matrix, under an air-liquid or grid-supported culture condition; the readout is invasion depth, invaded area, or an invasion index from histological or fluorescence images. This assay models stromal regulation of invasion because fibroblasts or CAFs remodel matrix, generate tracks, and can lead collective carcinoma-cell invasion; the resulting cancer-cell penetration into the gel reflects tumor-stroma-ECM interactions rather than migration on a rigid 2D substrate.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Matrigel/ECM Transwell Invasion Assay
The Matrigel/ECM Transwell invasion assay measures the ability of cells to move toward a chemoattractant while crossing an extracellular-matrix barrier placed on a porous membrane; therefore, the readout reflects both chemotactic motility and matrix invasion rather than migration alone. Matrigel is a basement-membrane-rich matrix derived from Engelbreth-Holm-Swarm mouse sarcoma and has been used as a reconstituted basement membrane barrier in chemoinvasion assays. The assay readout is generated by quantifying cells that reach the underside of the insert membrane or lower compartment after incubation, commonly by staining and counting invaded cells or by fluorescence-based quantification.
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3D Collagen/Hydrogel Matrix Invasion Assay
The 3D collagen/hydrogel matrix invasion assay is based on embedding cells within or on top of a three-dimensional fibrillar extracellular matrix (typically type I collagen or collagen-rich hydrogels) to model cell migration through a physiologically relevant physical barrier. In this system, invasive behavior is quantified by measuring the ability of cells to degrade, remodel, and migrate through the 3D matrix architecture, which better reflects in vivo tissue invasion compared to 2D migration assays. Collagen-based 3D matrices provide structural cues such as fiber alignment and porosity that influence cell motility and integrin-mediated adhesion, enabling observation of collective or single-cell invasion modes depending on matrix density and organization.
Purity & Documentation
References
[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. [Content Brief]
[2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5. [Content Brief]
[3]. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47. [Content Brief]
[4]. Liu X R, et al. UNC0638, a G9a inhibitor, suppresses epithelial‑mesenchymal transition‑mediated cellular migration and invasion in triple negative breast cancer[J]. Molecular medicine reports, 2018, 17(2): 2239-2244. [Content Brief]
[5]. Nualkaew T, et al. UNC0638 induces high levels of fetal hemoglobin expression in β-thalassemia/HbE erythroid progenitor cells[J]. Annals of hematology, 2020, 99: 2027-2036. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)