1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. HDAC-IN-92

HDAC-IN-92 is a pan-HDAC inhibitor with an IC50 of 12.58 µM in A2780 cells. HDAC-IN-92 demonstrates broad-spectrum, notable cytotoxic activity against a range of human cancer cell lines, including ovarian, liver, and breast carcinomas. HDAC-IN-92 causes apoptosis and demonstrates a notable decrease in tumor cell colony formation. HDAC-IN-92 inhibits the formation of blood vessels in the chick chorioallantoic membrane (CAM). HDAC-IN-92 exhibits anti-tumor effect in a 4T1 tumor-bearing mouse model. HDAC-IN-92 can be used for research targeting solid tumor.

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HDAC-IN-92

HDAC-IN-92 Chemical Structure

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Description

HDAC-IN-92 is a pan-HDAC inhibitor with an IC50 of 12.58 µM in A2780 cells. HDAC-IN-92 demonstrates broad-spectrum, notable cytotoxic activity against a range of human cancer cell lines, including ovarian, liver, and breast carcinomas. HDAC-IN-92 causes apoptosis and demonstrates a notable decrease in tumor cell colony formation. HDAC-IN-92 inhibits the formation of blood vessels in the chick chorioallantoic membrane (CAM). HDAC-IN-92 exhibits anti-tumor effect in a 4T1 tumor-bearing mouse model. HDAC-IN-92 can be used for research targeting solid tumor[1].

In Vitro

HDAC-IN-92 (compound 6g) (18 h) demonstrates significant cytotoxicity in a broad panel of cancer cell lines, with IC50s of 22.17 μM (MCF-7), 8.46 μM (HepG2), 8.10 μM (A2780), 26.89 μM (A2780cis), 75.90 μM (HT29), and 14.11 μM (4T1)[1].
HDAC-IN-92 (18 h) demonstrates a correlation between its cytotoxicity against cancer cells and its pan-HDAC inhibitory activity, suggesting that its antitumor effect may be mediated by the inhibition of histone deacetylases[1].
HDAC-IN-92 (8.10 μM, 24 h) significantly promotes apoptosis, increasing the total apoptotic population from 1.82 % to 22.17 %, and inhibits cell migration in A2780 cells[1].
HDAC-IN-92 (22.17 μM, 10 days) remarkably reduces colony formation in MCF-7 cancer cells[1].
HDAC-IN-92 (5 μM, 96 h) inhibits CAM angiogenesis as effectively as Vorinostat (HY-10221), as evidenced by a marked reduction in branching points, tube number, and total tube length[1].

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

Apoptosis Analysis[1]

Cell Line: A2780 cells
Concentration: 8.10 nM
Incubation Time: 24 h
Result: Increased percentage early and late apoptosis cells from 1.82 % of the control to 22.17 %.

Cell Proliferation Assay[1]

Cell Line: MCF-7 cells
Concentration: 22.17 nM
Incubation Time: 24 h
Result: Reduces colony formation in MCF-7 cancer cells.
In Vivo

HDAC-IN-92 (50 mg/kg, i.p., every other day for 21 days) inhibits tumor growth and is well-tolerated in 4T1 tumor-bearing BALB/c mouse model[1].

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

Animal Model: Female Balb/c mice (4-6 weeks old) injected subcutaneously with 4T1 cells[1]
Dosage: 50 mg/kg
Administration: i.p., every other day for 21 days
Result: Reduced tumor volume better than Vorinostat.
Exerted no significant effects on the body weight or survival rates of mice.
Induced tumor cell apoptosis without exhibiting toxicity in major organs.
Molecular Weight

384.43

Formula

C19H17FN4O2S

SMILES

O=C(NO)C1=CC=C(/N=C/C2=CN=C(SCC3=CC=CC(F)=C3)N2C)C=C1

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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.

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Product Name:
HDAC-IN-92
Cat. No.:
HY-175857
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