HDAC-IN-105
HDAC-IN-105 is a histone deacetylase (HDAC) inhibitor with binding to HDAC2 and HDAC4 isoforms. HDAC-IN-105 suppresses HDAC activity via binding within conserved HDAC catalytic pockets. HDAC-IN-105 induces G2/M phase cell cycle arrest. HDAC-IN-105 triggers mitochondrial dysfunction marked by loss of mitochondrial membrane potential. HDAC-IN-105 exhibits growth inhibition in triple-negative breast cancer cells and low toxicity toward normal cells. HDAC-IN-105 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C26H28BrN5O
- Molecular Weight:506.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HDAC2 |
HDAC4 |
HDAC-IN-105 (Compound 7e) (5-30 μM; 24 h) concentration-dependently reduces total cellular HDAC activity in MDA-MB-231 triple-negative breast cancer cells, with an apparent IC50 of 26.58 μM and a 63% reduction at 30 μM after 24 h of incubation[1].
HDAC-IN-105 (20-30 μM; 24 h) induces dose-dependent cytotoxic morphological changes in MDA-MB-231 triple-negative breast cancer cells after 24 h of incubation[1].
HDAC-IN-105 (10-100 μM; 24 h) exhibits potent antiproliferative activity with an IC50 of 27.59 μM in MDA-MB-231 cells, 34.18 μM in MCF-7 cells, 64.21 μM in HUVEC cells, and 105.23 μM in HDF cells[1].
HDAC-IN-105 (20-30 μM; 24 h) at 30 μM induces G2/M phase cell cycle arrest in MDA-MB-231 triple-negative breast cancer cells after 24 h of incubation, increasing the percentage of cells in G2/M phase from 20.6% to 33.2%[1].
HDAC-IN-105 (20-30 μM; 24 h) dose-dependently induces apoptosis in MDA-MB-231 triple-negative breast cancer cells after 24 h of incubation, increasing apoptotic cell percentage up to 24.5%[1].
HDAC-IN-105 (20-30 μM; 24 h) dose-dependently induces loss of mitochondrial membrane potential in MDA-MB-231 triple-negative breast cancer cells after 24 h of incubation, affecting up to 54% of cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:20 and 30 μM
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Incubation Time:24 h
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Result:Increased the percentage of cells in G2/M phase from 20.6% (control) to 19.5% with a corresponding increase in S phase to 30.9% at 20 μM.
Increased G2/M phase cells to 33.2% with S phase at 37.3% and G1 phase reduced to 29.5% at 30 μM.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:20 and 30 μM
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Incubation Time:24 h
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Result:Increased the percentage of apoptotic cells from 6.21% (control) to 13% at 20 μM.
Increased apoptotic cells to 24.5% at 30 μM.
Chemical Information
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Molecular Weight 506.44
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Formula C26H28BrN5O
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SMILES
BrC(C=C1)=CC=C1N2N=NC(COCCN(CC3)CCN3CC4=CC=C(C=CC=C5)C5=C4)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)