Zeprumetostat
Based on 1 publication(s) in Google Scholar
EZH2-IN-15 (SHR2554) is a EZH2 inhibitor. EZH2-IN-15 reduces the level of histone H3 lysine 27 trimethylation (H3K27me3), regulates gene expression and releases silenced tumor suppressor genes. EZH2-IN-15 induces cell apoptosis, alters cell cycle progression and downregulates cell cycle-related proteins. EZH2-IN-15 is applicable to research related to T-cell lymphoma.
For research use only. We do not sell to patients.
- Purity : 99.18%
- CAS No.: 2098545-98-1
- Formula: C32H44N4O4
- Molecular Weight:548.72
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Zeprumetostat
MoreAll Histone Methyltransferase Isoforms
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Biological Activity
Description
In Vitro
EZH2-IN-15 (SHR2554) (0.01, 0.1, 1, 5, 10, 50 μM; 144 h) inhibits the proliferation of H9, HH, HUT78, Karpas 299, and Jurkat TCL cell lines in a dose-dependent manner over 144 h, with IC50 values ranging from 0.365 to 5.810 μM[1].
EZH2-IN-15 (5, 10, 15 μM; 72 h) reduces H3K27me3 and EZH2 protein levels, induces pro-apoptotic protein expression, reduces anti-apoptotic protein expression, and downregulates cell cycle-related proteins in H9 and Karpas 299 TCL cell lines following 72 h of incubation at concentrations of 5, 10, or 15 μM[1].
EZH2-IN-15 (5, 10, 15 μM; 72 h) alters cell cycle distribution to increase G1-phase cell populations in H9 and Karpas 299 TCL cell lines following 72 h of incubation at concentrations of 5, 10, or 15 μM[1].
EZH2-IN-15 (5 μM; 72 h) modulates gene expression in H9 TCL cells following 72 h of incubation at 5 μM, with upregulated genes enriched in PI3K/AKT, MAPK, p53, and JAK-STAT signaling pathways, and activation of H3K27me3 target genes and HDAC1/HDAC2-downregulated genes[1].
EZH2-IN-15 (5, 8, 12, 15, 16, 17, 18, 19, 20, 24, 32, 36, 40 μM; 48 h) acts synergistically with Chidamide to inhibit proliferation of H9, HH, HUT78, Karpas 299, and Jurkat TCL cell lines following 48 h of co-incubation at fixed-ratio concentrations, as indicated by CI values < 1[1].
EZH2-IN-15 (8 μM (H9), 20 μM (Karpas 299); 48 h) reverses Tucidinostat (HY-109015)-induced elevations in H3K27me3 and synergistically enhances H3K27ac levels in H9 and Karpas 299 TCL cell lines following 48 h of co-incubation with 0.2 μM Chidamide at concentrations of 8 μM (H9) and 20 μM (Karpas 299)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H9 (cutaneous T-cell lymphoma, CTCL), HH (CTCL), HUT78 (CTCL), Karpas 299 (ALK+ anaplastic large T-cell lymphoma, ALCL), Jurkat (adult T-cell leukemia/lymphoma, ATLL)
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Concentration:0.01, 0.1, 1, 5, 10, 50 μM
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Incubation Time:144 h
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Result:Inhibited tumor cell proliferation in a dose-dependent manner, with 144-hour IC50 values of 0.365 μM for H9 cells, 0.443 μM for HH cells, 5.810 μM for HUT78 cells, 2.954 μM for Karpas 299 cells, and 3.001 μM for Jurkat cells.
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Cell Line:H9, Karpas 299 (T-cell lymphoma, TCL)
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Concentration:5, 10 μM (histone modification analysis); 5, 10, 15 μM (EZH2, apoptotic, and cell cycle-related protein analysis)
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Incubation Time:72 h
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Result:Reduced H3K27me3 levels in both H9 and Karpas 299 cells.
Decreased EZH2 protein expression in a dose-dependent manner, increased levels of the pro-apoptotic protein cleaved PARP, and decreased levels of the anti-apoptotic proteins XIAP and MCL1 in both cell lines.
Downregulated the expression of G1-phase associated proteins CDK4, CDK6, and S-phase associated protein CDK2 in both cell lines.
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Cell Line:H9, HH, HUT78, Karpas 299, Jurkat (T-cell lymphoma, TCL)
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Concentration:5, 8, 12, 15, 16, 17, 18, 19, 20, 24, 32, 36, 40 μM (fixed ratio with Chidamide)
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Incubation Time:48 h
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Result:Resulted in synergistic inhibition of tumor cell proliferation, with combination index (CI) values < 1 across all 5 TCL cell lines.
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Cell Line:H9, Karpas 299 (T-cell lymphoma, TCL)
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Concentration:8 μM (H9 cells), 20 μM (Karpas 299 cells) (co-incubated with 0.2 μM Chidamide)
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Incubation Time:48 h
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Result:Significantly diminished the Chidamide-induced increase in H3K27me3 levels in both H9 and Karpas 299 cells, while synergistically upregulating H3K27ac modification levels.
In Vivo
SHR2554 (50-100 mg/kg; p.o.; twice a day) significantly reduces tumor growth in a mouse ALK-negative ALCL PDX model, with enhanced efficacy when combined with Chidamide, and is well-tolerated by treated mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdc^scidIl2rg^tm1Sug/Jic (NCG) (female, 5-6 weeks old, subcutaneous T-cell lymphoma CDX model via H9 TCL cell inoculation)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; twice a day
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Result:Reduced tumor volume compared to control.
Achieved tumor inhibition rates of 50.9% (50 mg/kg + Chidamide) and 68.1% (100 mg/kg + Chidamide).
Significantly reduced tumor tissue H3K27me3 levels and Ki-67 proliferation marker intensity relative to control.
Caused no significant weight loss in mice treated alone or in combination.
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Animal Model:NOD.Cg-Prkdc^scidIl2rg^tm1Sug/Jic (NCG) (female, 5-6 weeks old, subcutaneous T-cell lymphoma PDX model via ALK-negative ALCL patient tumor tissue inoculation)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:p.o.; twice a day
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Result:Reduced tumor volume compared to control when administered as monotherapy.
Produced significantly greater tumor growth inhibition when combined with Chidamide than either single agent.
Caused no significant weight loss in mice treated alone or in combination.
- RT-PCR
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Real Time qPCR (Q-PCR)
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2098545-98-1
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Appearance Solid
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Molecular Weight 548.72
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Formula C32H44N4O4
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Color Off-white to yellow
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SMILES
O=C1NC(C)=CC(C)=C1CNC(C2=C3C=C(CN4CCCCC4)OC3=CC(N(C5CCOCC5)CC)=C2CC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
EZH2 inhibitor SHR2554 enhances the anti-tumor efficacy of HDAC inhibitor Chidamide through STAT1 in T-cell lymphoma. [Abstract]2025 Jul 14;16(1):522. PMID: 40659662
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (227.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (294 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 1 mM | 1.8224 mL | 9.1121 mL | 18.2242 mL | 45.5606 mL |
| 5 mM | 0.3645 mL | 1.8224 mL | 3.6448 mL | 9.1121 mL | |
| 10 mM | 0.1822 mL | 0.9112 mL | 1.8224 mL | 4.5561 mL | |
| 15 mM | 0.1215 mL | 0.6075 mL | 1.2149 mL | 3.0374 mL | |
| 20 mM | 0.0911 mL | 0.4556 mL | 0.9112 mL | 2.2780 mL | |
| 25 mM | 0.0729 mL | 0.3645 mL | 0.7290 mL | 1.8224 mL | |
| 30 mM | 0.0607 mL | 0.3037 mL | 0.6075 mL | 1.5187 mL | |
| 40 mM | 0.0456 mL | 0.2278 mL | 0.4556 mL | 1.1390 mL | |
| 50 mM | 0.0364 mL | 0.1822 mL | 0.3645 mL | 0.9112 mL | |
| 60 mM | 0.0304 mL | 0.1519 mL | 0.3037 mL | 0.7593 mL | |
| 80 mM | 0.0228 mL | 0.1139 mL | 0.2278 mL | 0.5695 mL | |
| 100 mM | 0.0182 mL | 0.0911 mL | 0.1822 mL | 0.4556 mL |
Zeprumetostat Related Classifications
HY-153191 Related Classifications
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