2. Epigenetics
  3. Histone Methyltransferase
  4. UNC0379 TFA

UNC0379 TFA 

Cat. No.: HY-12335A
COA Handling Instructions

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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2 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of UNC0379 TFA:

Top Publications Citing Use of Products

    UNC0379 TFA purchased from MCE. 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.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT8

    • 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].

    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].

    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

    Appearance

    Solid

    Formula

    C25H36F3N5O4
    CAS No.
    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
    10 mM 0.1895 mL 0.9477 mL 1.8954 mL
    *Please refer to the solubility information to select the appropriate solvent.
    Purity & Documentation

    Purity: 99.91%

    COA (251 KB)

    Handling Instructions (2659 KB)
    References
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    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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    Keywords:

    UNC03791620401-83-3UNC 0379UNC-0379Histone MethyltransferaseOvarian cancerlysine methyltransferaseantitumorHGSOCOVCAR3JHOS3neuroblastomapulmonary fibrosisInhibitorinhibitorinhibit

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