1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis Bcl-2 Family CDK
  3. HDAC-IN-51

HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer.

For research use only. We do not sell to patients.

HDAC-IN-51

HDAC-IN-51 Chemical Structure

CAS No. : 3026728-28-6

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Description

HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer[1].

IC50 & Target[1]

HDAC10

0.32 μM (IC50)

HDAC1

0.353 μM (IC50)

HDAC2

0.431 μM (IC50)

HDAC3

0.515 μM (IC50)

HDAC11

85.4 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.51 μM
Compound: 8d; MC2666
Antiproliferative activity against human A549 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 36549114]
HCT-116 IC50
0.32 μM
Compound: 8d; MC2666
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 36549114]
K562 IC50
0.32 μM
Compound: 8d; MC2666
Antiproliferative activity against human K562 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human K562 cells incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 36549114]
In Vitro

HDAC-IN-51 (compound 8d; 1 nM-10 μM; 48 h) has antiproliferative activity with IC50 values of 0.54, 0.56, and 1.35 μM for K562, HCT116, and A549 cells, respectively[1].
HDAC-IN-51 (1 and 5 μM; 24 and 48 h; U937 leukaemia cells) arrests cell cycle at the G1 phase[1].
HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) induces apoptosis and down-regulates miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p)[1].
HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) increases mRNA expression of p21, BAX and BAK, down-regulates cyclin D1 and BCL-2[1].

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

Cell Viability Assay[1]

Cell Line: K562, HCT116, and A549 cells
Concentration: 1 nM-10 μM
Incubation Time: 48 hours
Result: Inhibited cell growth in cancer cells.

Cell Cycle Analysis[1]

Cell Line: U937 leukaemia cells
Concentration: 1 and 5 μM
Incubation Time: 24 and 48 hours
Result: Blocked the cell cycle at the G1 phase in U937 leukaemia cells.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 1 and 5 μM
Incubation Time: 48 hours
Result: Down-regulates miRNAs with antiapoptotic activity including miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 1 and 5 μM
Incubation Time: 48 hours
Result: Increased mRNA expression of p21, BAX and BAK and down-regulated cyclin D1 and BCL-2 in a dose-dependent manner.
Molecular Weight

436.51

Formula

C27H24N4O2

CAS No.
SMILES

NC1=CC=CC=C1NC(C2=NC=C(C=C2)NC(C(C3=CC=CC=C3)CC4=CC=CC=C4)=O)=O

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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    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.

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HDAC-IN-51
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HY-152173
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