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.
For research use only. We do not sell to patients.
- Formula: C29H36BrN7O4
- Molecular Weight:626.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
|
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) |
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.
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Cell Line:SU-DHL-6, MOLM-13, OCI-AML2, MV4-11, U937 and OCI-AML3
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Concentration:0.1, 1, 5, 10, 100 μM
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Incubation Time:48, 120 h
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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).
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Cell Line:MOLM13 cells
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Concentration:4 μM
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Incubation Time:6 h
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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.
Chemical Information
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Molecular Weight 626.54
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Formula C29H36BrN7O4
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDACs/EZH2-IN-1 Related Classifications
HY-169400 Related Classifications
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