1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. HDAC-IN-46

HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC).

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HDAC-IN-46 Chemical Structure

HDAC-IN-46 Chemical Structure

CAS No. : 2562386-85-8

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Description

HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

HDAC1

0.21 μM (IC50)

HDAC6

0.021 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
88.46 μM
Compound: 12c
Antiproliferative activity in human A549 cells assessed as inhibition of cell viability after 72 hrs by MTS assay
Antiproliferative activity in human A549 cells assessed as inhibition of cell viability after 72 hrs by MTS assay
[PMID: 32061484]
MCF7 IC50
83.34 μM
Compound: 12c
Antiproliferative activity in human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTS assay
Antiproliferative activity in human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTS assay
[PMID: 32061484]
MDA-MB-231 IC50
21.4 μM
Compound: 12c
Antiproliferative activity in human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by MTS assay
Antiproliferative activity in human MDA-MB-231 cells assessed as inhibition of cell viability after 72 hrs by MTS assay
[PMID: 32061484]
In Vitro

HDAC-IN-46 (compound 12c) has antiproliferative activity against MDA-MB-231, A549 and MCF-7 with IC50s of 88.46±10.5 μM, 83.34 ± 15.5 μM and 21.4±3.7 μM, respectively[1].
HDAC-IN-46 (5, 12.5 and 25 μM; 24 h) causes concentration-dependent upregulation of p-p38 and downregulation of Bcl-xL and cyclin D1 in MDA-MB-231 cells[1].
HDAC-IN-46 (12.5 and 25 μM; 48 h) induces significant G2 phase arrest and apoptosis[1].

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

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 5, 12.5 and 25 μM
Incubation Time: 24 h
Result: Caused concentration-dependent upregulation of p-p38 and downregulation of Bcl-xL and cyclin D1.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 and 25 μM
Incubation Time: 48 h
Result: Induced significant G2 phase arrest and apoptosis.
Molecular Weight

438.53

Formula

C22H30N8O2

CAS No.
SMILES

O=C(NO)CCCCCCCN1N=NC(C2=CC=C(C3=C(CC)N=C(N)N=C3N)C=C2)=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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HDAC-IN-46
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HY-150597
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