2. Epigenetics
  3. Histone Methyltransferase
  4. UNC0379

UNC0379 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 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 Chemical Structure

UNC0379 Chemical Structure

CAS No. : 1620401-82-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 25 In-stock
5 mg USD 60 In-stock
10 mg USD 100 In-stock
50 mg USD 300 In-stock
100 mg USD 450 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of UNC0379:

UNC0379 Related Antibodies

Top Publications Citing Use of Products

    UNC0379 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.

    View All Histone Methyltransferase Isoform Specific Products:

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    UNC0379 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 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma[1][2][3].

    IC50 & Target

    SETD8/KMT5A

     

    In Vitro

    UNC0379 (1-10 μM, 9 days) inhibits HGSOC cells proliferation[2].
    ? UNC0379 (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells[2].
    ? UNC0379 (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.

    UNC0379 Related Antibodies

    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 (intratracheal administration, 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

    413.56

    Formula

    C23H35N5O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    COC1=C(OC)C=C2C(N=C(N3CCCC3)N=C2NCCCCCN4CCCC4)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (120.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4180 mL 12.0901 mL 24.1803 mL
    5 mM 0.4836 mL 2.4180 mL 4.8361 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.90%

    COA (248 KB) LCMS (264 KB)

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4180 mL 12.0901 mL 24.1803 mL 60.4507 mL
    5 mM 0.4836 mL 2.4180 mL 4.8361 mL 12.0901 mL
    10 mM 0.2418 mL 1.2090 mL 2.4180 mL 6.0451 mL
    15 mM 0.1612 mL 0.8060 mL 1.6120 mL 4.0300 mL
    20 mM 0.1209 mL 0.6045 mL 1.2090 mL 3.0225 mL
    25 mM 0.0967 mL 0.4836 mL 0.9672 mL 2.4180 mL
    30 mM 0.0806 mL 0.4030 mL 0.8060 mL 2.0150 mL
    40 mM 0.0605 mL 0.3023 mL 0.6045 mL 1.5113 mL
    50 mM 0.0484 mL 0.2418 mL 0.4836 mL 1.2090 mL
    60 mM 0.0403 mL 0.2015 mL 0.4030 mL 1.0075 mL
    80 mM 0.0302 mL 0.1511 mL 0.3023 mL 0.7556 mL
    100 mM 0.0242 mL 0.1209 mL 0.2418 mL 0.6045 mL
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    UNC0379 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:

    UNC03791620401-82-2UNC 0379UNC-0379Histone MethyltransferaseOvarian cancerlysine methyltransferaseantitumorHGSOCOVCAR3JHOS3neuroblastomapulmonary fibrosisInhibitorinhibitorinhibit

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