EZM0414
Based on 10 publication(s) in Google Scholar
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
For research use only. We do not sell to patients.
- Purity: 99.11%
- CAS No.: 2411748-50-8
- Formula: C22H29FN4O2
- Molecular Weight:400.49
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) EZM0414
More- Cell. 2026 Jun 11;189(12):3541-3552.e18. [Abstract]
- Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9. [Abstract]
- Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
- Int J Biol Macromol. 2024 Oct 28:136767. [Abstract]
- Cell Rep. 2025 Jan 15;44(1):115219. [Abstract]
- Transl Psychiatry. 2026 Apr 1;16(1):275. [Abstract]
- Cancer Sci. 2026 May 22. [Abstract]
- Sci Rep. 2024 Jun 3;14(1):12728. [Abstract]
- Anim Reprod Sci. 2026 May 5;292:108229.
- Research Square Preprint. 2023 May 26.
Customer Validation & Images
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Others
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Cell Proliferation/Viability Assay
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WB
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WB
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Others
All Histone Methyltransferase Isoforms
More
Biological Activity
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SETD2/KMT3A |
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Cell Line
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Type | Value | Description | References |
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| KMS-11 | IC50 |
370 nM
Compound: EZM0414
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Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay
Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay
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[PMID: 35859865] |
EZM0414 inhibits proliferation of a panel of MM and DLBCL cell lines, with IC50s of 0.24 μM for t(4;14) cell, 0.023 μM- >10 μM for DLBCL cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
EZM0414 (50 mg/kg, p.o.) shows almost 100% oral bioavailability in rats and mice, t1/2 of 1.8 h (mice)and 3.8 h (rats)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2411748-50-8
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Appearance Solid
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Molecular Weight 400.49
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Formula C22H29FN4O2
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Color Off-white to light yellow
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SMILES
FC1=C2C(NC(C(N[C@H]3C[C@](N4CCN(CC4)C(C)=O)([H])CCC3)=O)=C2)=C(C=C1)C
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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 and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
Cell Stem Cell
Highly efficient and rapid generation of human pluripotent stem cells by chemical reprogramming. [Abstract]2023 Apr 6;30(4):450-459.e9. PMID: 36944335
EZM0414 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9. [Abstract]
Number of hCiPSC colonies induced from hASFs (hASFs-38040) (n = 3) and hADSCs (hADSCs-0618) (n = 4) with stage I condition (SI) or SI plus EZM0414 TFA (SET: 0.2 μM) using a three-stage protocol.
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Nat Chem Biol
2023 Sep;19(9):1105-1115. PMID: 36973442
EZM0414 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Bar plots showing cell proliferation in the presence of EZM0414 TFA (SETD2-IN-1) at 0.1, 1, or 10 μM after 21-day treatment.
EZM0414 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Immunoblot showing H3K27me3 and H3K36me3 levels in lymphoma cell lines treated with 5 μM EZM0414 TFA (SETD2-IN-1) for 72 h.
EZM0414 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Immunoblot showing γH2AX and H3K36me3 levels in Karpas-422 treated with 5 μM EZM0414 TFA (SETD2-IN-1) for 10 days or 10 μM etoposide for 24 h.
EZM0414 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Aggregate profile plot of wild-type Karpas-422 H3K36me3 ChIP-Rx signal (y-axis) for EZM0414 TFA (SETD2-IN-1: 5 μM) treatment centered around H3K36me3 domains in wild-type cells (x-axis).
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Int J Biol Macromol
SETD2 deficiency in peripheral sensory neurons induces allodynia by promoting NMDA receptor expression through NFAT5 in rodent models. [Abstract]2024 Oct 28:136767. PMID: 39476923 -
Cell Rep
Menin orchestrates macrophage reprogramming to maintain the pulmonary immune homeostasis. [Abstract]2025 Jan 15;44(1):115219. PMID: 39817905 -
Transl Psychiatry
Non-gene-edited neural stem cells reverse neuroinflammation and microbiota dysbiosis in a sprague-dawley rat model of autism spectrum disorder. [Abstract]2026 Apr 1;16(1):275. PMID: 41922322 -
Cancer Sci
Blocking SETD2 Enhances the Therapeutic Efficiency of Menin Inhibitor in MLL-Fusion Leukemia. [Abstract]2026 May 22. PMID: 42170936 -
Sci Rep
SPA inhibits hBMSC osteogenic differentiation and M1 macrophage polarization by suppressing SETD2 in acute suppurative osteomyelitis. [Abstract]2024 Jun 3;14(1):12728. PMID: 38830934 -
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Solvent & Solubility
DMSO : 120 mg/mL (299.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 and light). 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 (sealed storage, away from moisture and light). 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 (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (sealed storage, away from moisture and light). 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 | 2.4969 mL | 12.4847 mL | 24.9694 mL | 62.4235 mL |
| 5 mM | 0.4994 mL | 2.4969 mL | 4.9939 mL | 12.4847 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4969 mL | 6.2424 mL | |
| 15 mM | 0.1665 mL | 0.8323 mL | 1.6646 mL | 4.1616 mL | |
| 20 mM | 0.1248 mL | 0.6242 mL | 1.2485 mL | 3.1212 mL | |
| 25 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4969 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8323 mL | 2.0808 mL | |
| 40 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5606 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0404 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 mL | |
| 100 mM | 0.0250 mL | 0.1248 mL | 0.2497 mL | 0.6242 mL |
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