2. Epigenetics
  3. Histone Methyltransferase
  4. EZM0414

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.

CAS No. : 2411748-50-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of EZM0414:

EZM0414 Related Antibodies

Top Publications Citing Use of Products

    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.

    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).

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1].

    IC50 & Target

    SETD2/KMT3A

     

    Cellular Effect
    Cell Line Type Value Description References
    KMS-11 IC50
    370 nM
    Compound: EZM0414
    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
    		[PMID: 35859865]
    In Vitro

    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 Related Antibodies
    In Vivo

    EZM0414 (15 and 30 mg/kg, p.o., BID, daily, ) inhibits tumor growth in NOD SCID mouse xenograft model implanted with human KMS-11 cells, and is well-tolerated[3].
    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.
    Molecular Weight

    400.49

    Formula

    C22H29FN4O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    FC1=C2C(NC(C(N[C@H]3C[C@](N4CCN(CC4)C(C)=O)([H])CCC3)=O)=C2)=C(C=C1)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    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)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4969 mL 12.4847 mL 24.9694 mL
    5 mM 0.4994 mL 2.4969 mL 4.9939 mL
    View the 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.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Purity & Documentation
    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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    EZM0414 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    EZM04142411748-50-8EZM 0414EZM-0414Histone Methyltransferaserelapsed or refractory multiple myelomadiffuse large B-cell lymphomaSETD2oralDLBCLInhibitorinhibitorinhibit

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