2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC Histone Methyltransferase
  4. HDACs/EZH2-IN-1

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.

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HDACs/EZH2-IN-1 Chemical Structure

HDACs/EZH2-IN-1 Chemical Structure

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HDACs/EZH2-IN-1 Related Antibodies

Top Publications Citing Use of Products

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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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

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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].

IC50 & Target[1]

HDAC1

0.23 μM (IC50)

HDAC6

0.07 μM (IC50)

HDAC4

>10 μM (IC50)

HDAC11

>10 μM (IC50)

EZH2 WT

0.84 nM (IC50)

EZH2 Y641N

1.36 nM (IC50)

In Vitro

HDACs/EZH2-IN-1 (5 μM, 48-120 h) displays strong antiproliferative activities against SU-DHL-6 cells, which is a DLBCL cell line harboring EZH2 Y641N mutation, with IC50 of 1.04 μM (48 h) and 0.17 μM (120 h)[1].
HDACs/EZH2-IN-1 (0.1-100 μM 48 h) inhibits the growth of AML cells, with IC50 of 1.39 μM (MV4-11), 2.45 μM (U937), and 1.32 μM (OCI-AML3)[1].
HDACs/EZH2-IN-1 (4 μM, 6 h) increases the intracellular levels of the HDAC1/2/3 substrate acetylhistone H3 (AC-HH3) and the HDAC6 substrate acetyl-α-tubulin (AC-α-tubulin) [1].
HDACs/EZH2-IN-1 (2 μM, 48 h) induces differentiation of MOLM13 cells, with increasing expression of two myeloid maturation markers CD11b and CD14[1].
HDACs/EZH2-IN-1 (2-4 μM, 48 h) induces apoptosis of MOLM13 cells dose-dependently[1].
HDACs/EZH2-IN-1 (1-2 μM) synergizes with anti-AML compounds (Cytarabine (HY-13605), Daunorubicin (HY-13062A), Gilteritinib (HY-12432)) against cancer in MOLM13 cells[1].
HDACs/EZH2-IN-1 shows good metabolic stability in human and rat plasma, with T1/2 of >180 and 138 min, respectively[1].

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

HDACs/EZH2-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: SU-DHL-6, MOLM-13, OCI-AML2, MV4-11, U937 and OCI-AML3
Concentration: 0.1, 1, 5, 10, 100 μM
Incubation Time: 48, 120 h
Result: Displayed strong antiproliferative activities against SU-DHL-6 cells (5 μM, 48 h and 120 h).
Inhibited the growth of cell lines, with IC50 of 1.39 μM (MV4-11), 2.45 μM (U937), and 1.32 μM (OCI-AML3) (1, 10, 100 μM, 48 h).

Western Blot Analysis[1]

Cell Line: MOLM13 cells
Concentration: 4 μM
Incubation Time: 6 h
Result: Increased the intracellular levels of the HDAC1/2/3 substrate acetylhistone H3 (AC-HH3) and the HDAC6 substrate acetyl-α-tubulin (AC-α-tubulin).
Led to a significant reduction in the levels of trimethylation at H3K27.
Molecular Weight

626.54

Formula

C29H36BrN7O4
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HDACs/EZH2-IN-1 Related Classifications

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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.

Keywords:

HDACs/EZH2-IN-1HDACHistone MethyltransferaseHistone deacetylasesAnticancerDual inhibitorAMLDLBCLDifferentiationAntiproliferativeInhibitorinhibitorinhibit

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