1. Epigenetics
  2. Histone Methyltransferase
  3. EPZ031686

EPZ031686 

Cat. No.: HY-19324 Purity: 99.60%
COA Handling Instructions

EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research.

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

EPZ031686 Chemical Structure

EPZ031686 Chemical Structure

CAS No. : 1808011-22-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 546 Get quote
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 546 Get quote
Solid
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    EPZ031686 purchased from MCE. Usage Cited in: Aging. 2020 Nov 3;12(21):21423-21445.  [Abstract]

    EPZ031686 (20 μM) reverses Ang II-induced PARP16 and RAECs senescence. Inhibition of Smyd3 could downregulate protein level of PARP16, together with reduced ER stress and senescence markers.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research[1].

    IC50 & Target[1]

    SMYD3

    3 nM (IC50)

    In Vivo

    EPZ031686 (1-50 mg/mL; p.o. and i.v.; Male CD-1 mice) has good bioavailability following oral dosing in mice[1].

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

    Animal Model: Male CD-1 mice[1]
    Dosage: 1, 5 and 50 mg/kg
    Administration: Oral administration and intravenous injection
    Result: 1.19
    parameter 1 mg/kg i.v. 5 mg/kg p.o. 50 mg/kg p.o.
    CL (mL/min/kg) 27
    CLr (mL/min/kg) 5.3
    Vss (L/kg) 2.3
    t1/2 (h) 1.7 2.7 2.2
    tmax (h) 0.89 1.3
    Cmax (ng/mL) 345 4693
    AUC0-last (h·ng/mL) 603 1281 21158
    AUC0-inf (h·ng/mL) 616 1479 21170
    Molecular Weight

    591.09

    Formula

    C26H34ClF3N4O4S

    CAS No.
    SMILES

    O=C(C1)NC2=C1C=C(C(N[[email protected]@H]3C[[email protected]]4N(S(CC5CCN(CCCC(F)(F)F)CC5)(=O)=O)[[email protected]](CC4)C3)=O)C(Cl)=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 35 mg/mL (59.21 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6918 mL 8.4589 mL 16.9179 mL
    5 mM 0.3384 mL 1.6918 mL 3.3836 mL
    10 mM 0.1692 mL 0.8459 mL 1.6918 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  30% PEG300  70% (20% SBE-β-CD in saline)

      Solubility: 10 mg/mL (16.92 mM); Suspended solution; Need ultrasonic and warming

    • 2.

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

      Solubility: ≥ 1.75 mg/mL (2.96 mM); Clear solution

    • 3.

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

      Solubility: ≥ 1.75 mg/mL (2.96 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1.75 mg/mL (2.96 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.71%

    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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    Product Name:
    EPZ031686
    Cat. No.:
    HY-19324
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