1. Epigenetics
  2. Histone Methyltransferase
  3. UNC0379 TFA

UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.

For research use only. We do not sell to patients.

UNC0379 TFA Chemical Structure

UNC0379 TFA Chemical Structure

CAS No. : 1620401-83-3

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Top Publications Citing Use of Products

    UNC0379 TFA purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.  [Abstract]

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma[1][2][3].

    IC50 & Target

    SETD8 (KMT5A)[1]

    In Vitro

    UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation[2].
    UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells[2].
    UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1]

    Cell Line: JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu
    Concentration: 1-10 μM
    Incubation Time: 9 days
    Result: Inhibited HGSOC cells proliferation with IC50s ranging from 0.39 to 3.20 µM.

    Cell Cycle Analysis[1]

    Cell Line: JHOS3, OVCAR3
    Concentration: 10 µM
    Incubation Time: 96 h
    Result: Arrested cells in sub-G1 phase.
    In Vivo

    UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Bleomycin (BLM)-induced lung fibrosis mouse model[3]
    Dosage: 1 mg/kg/day
    Administration: Intratracheal administration, on day7, 8, and 9.
    Result: Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation.
    Molecular Weight

    527.58

    Formula

    C25H36F3N5O4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

    COC1=C(OC)C=C2C(N=C(N3CCCC3)N=C2NCCCCCN4CCCC4)=C1.O=C(O)C(F)(F)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (189.54 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8954 mL 9.4772 mL 18.9545 mL
    5 mM 0.3791 mL 1.8954 mL 3.7909 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    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
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.91%

    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). 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
    H2O 1 mM 1.8954 mL 9.4772 mL 18.9545 mL 47.3862 mL
    5 mM 0.3791 mL 1.8954 mL 3.7909 mL 9.4772 mL
    10 mM 0.1895 mL 0.9477 mL 1.8954 mL 4.7386 mL
    15 mM 0.1264 mL 0.6318 mL 1.2636 mL 3.1591 mL
    20 mM 0.0948 mL 0.4739 mL 0.9477 mL 2.3693 mL
    25 mM 0.0758 mL 0.3791 mL 0.7582 mL 1.8954 mL
    30 mM 0.0632 mL 0.3159 mL 0.6318 mL 1.5795 mL
    40 mM 0.0474 mL 0.2369 mL 0.4739 mL 1.1847 mL
    50 mM 0.0379 mL 0.1895 mL 0.3791 mL 0.9477 mL
    60 mM 0.0316 mL 0.1580 mL 0.3159 mL 0.7898 mL
    80 mM 0.0237 mL 0.1185 mL 0.2369 mL 0.5923 mL
    100 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4739 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    UNC0379 TFA 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.

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    UNC0379 TFA
    Cat. No.:
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