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HDACs/EZH2-IN-1

HDACs/EZH2-IN-1

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SKU:QM-0154276

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  • Description

    HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively) . HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis[1].

  • Molecular Formula

    C29H36BrN7O4

  • Molecular Weight

    626.54

  • Smiles

    BrC1=CC(N(CC2CCN(CC2)C3=NC=C(C=N3)C(NO)=O)CC)=C(C(C(NCC4=C(C=C(NC4=O)C)C)=O)=C1)C

  • Target

    Apoptosis; HDAC; Histone Methyltransferase

  • Isoform

    EZH2; HDAC1; HDAC11; HDAC4; HDAC6

  • Shipping Conditions

    Room temperature

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HDACs/EZH2-IN-1

HDACs/EZH2-IN-1 (Compound 22a) is a certified reference standard supplied by Quantimol for laboratory and scientific research.

HDACs/EZH2-IN-1 is a potent dual inhibitor of histone deacetylases (HDACs) and the histone methyltransferase EZH2. It inhibits EZH2 Y641N with a 98% inhibition rate at 50 nM, and selectively inhibits HDAC1 (IC50: 0.23 μM) and HDAC6 (IC50: 0.07 μM). This compound exerts antiproliferative effects on diffuse large B-cell lymphoma (DLBCL) cells harbouring EZH2 mutations and on various acute myeloid leukaemia (AML) cell lines, and induces cell differentiation and apoptosis.

Key properties:

  • Targets: HDAC1, HDAC6, EZH2 (dual epigenetic inhibitor)
  • EZH2 Y641N inhibition: 98% at 50 nM
  • HDAC1 IC50: 0.23 μM | HDAC6 IC50: 0.07 μM
  • Purity: ≥98% (HPLC)
  • Storage: -20°C, protected from light
  • Solubility: DMSO (recommended)

Applications: Epigenetic cancer research, DLBCL and AML biology, HDAC/EZH2 dual inhibition studies, apoptosis and differentiation assays, lymphoma drug discovery.

Supplied by Quantimol as a certified reference standard for research use only. Not for human or veterinary use.