1. Epigenetics
  2. Histone Methyltransferase

EPZ031686 

Cat. No.: HY-19324 Purity: 99.63%
Handling Instructions

EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.

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
10 mM * 1 mL in DMSO USD 546 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively. In vitro: EPZ031686 have a cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. The first SMYD3 inhibitor identify to show double-digit nanomolar cellular activity. EPZ031686 show < 30% inhibition against 16 histone methyltransferase targets at a 10 uM screening concentration. In vivo: EPZ031686 show good bioavailability following oral dosing in mice. The administration for mice is 1 mg/kg by i.v.

References
Preparing Stock Solutions
Concentration Volume 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.
References
Molecular Weight

591.09

Formula

C₂₆H₃₄ClF₃N₄O₄S

CAS No.

1808011-22-4

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 5.9 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.63%

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