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 Chemical Structure

HDAC-IN-57 Chemical Structure

CAS No. : 2716217-79-5

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HDAC-IN-57 Related Antibodies

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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)

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

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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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  • 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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