2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis Histone Demethylase
  4. HDAC-IN-57

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity.

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HDAC-IN-57

HDAC-IN-57 Chemical Structure

CAS No. : 2716217-79-5

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HDAC-IN-57 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

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

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Description

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity[1].

IC50 & Target[1]

HDAC1

2.07 nM (IC50)

HDAC2

4.71 nM (IC50)

HDAC6

2.4 nM (IC50)

HDAC8

107 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.48 μM
Compound: 5e
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
GES1 IC50
8.66 μM
Compound: 5e
Cytotoxicity against human GES1 cells harboring low LSD1 expression assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Cytotoxicity against human GES1 cells harboring low LSD1 expression assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
HCT-116 IC50
0.57 μM
Compound: 5e
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
MGC-803 IC50
0.45 μM
Compound: 5e
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
MOLT-4 IC50
0.25 μM
Compound: 5e
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
MV4-11 IC50
0.14 μM
Compound: 5e
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
THP-1 IC50
0.47 μM
Compound: 5e
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay
[PMID: 37086699]
In Vitro

HDAC-IN-57 (Compound 5e) (1.0 μM, 2.5 μM, 5.0 μΜ；48 hour) inhibits migration and invasion activity of MGC-803 and HCT-116 cells[1].
HDAC-IN-57 (1.0 μM, 2.5 μM, 5.0 μΜ；48 hour) significantly inhibits the growth of solid tumor cell lines MGC-803, A549, and HCT-116, with IC50s of 0.45 μM. 1.48 μM and 0.57 μM, respectively[1].
HDAC-IN-57 (1.0 μM. 2.5 μM, 5.0 μΜ; 48 hours) triggers apoptosis of MGC-803 and HCT -116 cells in a dose-dependent manner[1].
HDAC-IN-57 (1.0 μM. 2.5 μM, 5.0 μΜ; 48 hours) inhibits LSD1 and HDACs of MGC-803 and HCT -116 cells[1].
HDAC-IN-57 (1.0 μM. 2.5 μM, 5.0 μΜ; 48 hours) induces G2/M cycle arrest in MGC-803 and HCT-116 cells[1].
HDAC-IN-57 (Compound 5e) showes excellent metabolic stability in human liver (HLM) and rat liver microsomes (RLM), maintaining 86.1% and 87.4%, respectively, of the parent compound after incubation for 1 h, with T1/2 values over 120 min[1].

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

HDAC-IN-57 Related Antibodies

Western Blot Analysis[1]

Cell Line: MGC-803 cells, HCT-116 cells
Concentration: 1.5 μM
Incubation Time: 48 hours
Result: Inhibited cellular LSD1 and HDACs.
Upregulated the expression of apoptotic markers, including cytochrome C, Bax, cleaved caspase-3/7/9, and cleaved PARP, while downregulating the expression of anti-apoptotic protein Bcl-2.

Apoptosis Analysis[1]

Cell Line: MGC-803 cells, HCT-116 cells
Concentration: 1.0 μM, 2.5 μM, 5.0 μM
Incubation Time: 48 hours
Result: Triggered MGC-803 and HCT116 cells apoptosis in a dose-dependent manner.
Induced about 55.4% and 51.5% MGC-803 cell apoptosis at a concentration of 5 μM.

Cell Migration Assay [1]

Cell Line: MGC-803 cells, HCT-116 cells
Concentration: 1.0 μM, 2.0 μM, 4 μM
Incubation Time: 48 hours
Result: Reduced the number of migrated of MGC-803 and HCT-116 cells. Inhibited the migration and invasion of cancer cells.

Cell Cycle Analysis[1]

Cell Line: MGC-803 cells, HCT-116 cells
Concentration: 1.0 μM, 2.5 μM, 5.0 μM
Incubation Time: 48 hours
Result: Induced G2/M cycle arrest in MGC-803 and HCT-116 cells.
In Vivo

HDAC-IN-57 (Compound 5e) (1 mg.kg for i.v., 10 mg/kg for p.o.) shows a T1/2 of 0.37 h (i.v.) and 2.75 h (p.o.), and oral bioavailability (F%) of 10.6%[1].
HDAC-IN-57 (25 or 50 mg/kg, oral gavage once daily for 21 consecutive days) achieves a dose-dependent inhibition for tumor growth in an MGC-803 xenograft model with NOD-SCID mice[1].
.

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

Animal Model: MGC-803 xenograft model in NOD-SCID mice[1]
Dosage: 25 or 50 mg/ kg
Administration: Oral gavage (p.o.);
Result: Achieved a dose-dependent tumor growth inhibition (TGI) of 44.8% at 25 mg/kg and 71.5% at 50 mg/kg.
Animal Model: Male SD rats (Pharmacokinetic assay)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: Intravenous injection (i.v.); Oral gavage (p.o.)
Result: Pharmacokinetic parameters for HDAC-IN-57 (Compound 5e) in SD rats[1]
Route Dose (mg/kg) T1/2 (h) Tmax (h) CL (mL•min-1/kg-1) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) Cmax (ng/mL) VZ (L/kg) F (%)
i.v. 1 0.37 / 1.61 644.1 645.8 1892.8 0.82 /
p.o. 10 2.75 0.25 / 685.2 766.2 716.4 52.2 10.6
Molecular Weight

377.39

Formula

C21H19N3O4
CAS No.
SMILES

O=C(C1=CC=C(CNC(C2=CC(C3=CC=C(OC)C=C3)=NC=C2)=O)C=C1)NO
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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HDAC-IN-57 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:

HDAC-IN-572716217-79-5HDACApoptosisHistone DemethylaseHistone deacetylasesHDAC1 inhibitoranti-tumorMGC-803HCT-116xenograft modelsInhibitorinhibitorinhibit

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