FF2039
FF2039 is a pan-HDAC PROTAC degrader that binds to DCAF11, acting on HDAC6, HDAC1, HDAC2 and HDAC4. FF2039 recruits the DCAF11 E3 ligase and mediates the polyubiquitination and degradation of HDACs via the ubiquitin-proteasome system. FF2039 induces cell cycle arrest, apoptosis, cytotoxicity and antiproliferative activity in cancer cells, and reduces the clonogenic capacity of cancer cells. FF2039 is applicable to research related to multiple myeloma, triple-negative breast cancer and glioblastoma.
(Pink: HDAC1 and HDAC2 and HDAC4 and HDAC6 ligand (HY-168864); Blue: Ligands for E3 Ligase ligand (HY-W957284); Black: linker (HY-W881439)).
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- Formule: C43H56Cl3N5O6
- Masse moléculaire:845.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
HDAC1 1.03 μM (IC50) |
HDAC2 2.15 μM (IC50) |
HDAC4 12.4 μM (IC50) |
HDAC6 0.053 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | EC50 |
28 μM
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Antiproliferative activity against triple negative breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability assay.
Antiproliferative activity against triple negative breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell viability assay.
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39973224 |
| U-87MG ATCC | EC50 |
30 μM
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Antiproliferative activity against glioblastoma U-87MG cells assessed as reduction in cell viability incubated for 72 hrs by cell viability assay.
Antiproliferative activity against glioblastoma U-87MG cells assessed as reduction in cell viability incubated for 72 hrs by cell viability assay.
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39973224 |
In Vitro
FF2039 (10 μM; 24 h) reduces HDAC1 levels by 71% and induces significant degradation of HDAC6 in MM.1S cells. It binds HDAC6 and class I HDACs in MM.1S cells, inducing hyperacetylation of α-tubulin and histone H3. It also induces significant degradation of HDAC1 and HDAC6 in U-87MG cells, with degradation efficacy weaker than that observed in MM.1S cells[1].
FF2039 (10 μM; 24 h) acts as a pan-HDAC degrader in MM.1S cells, achieving a maximum degradation rate of 90% for HDAC1 and 71%-76% for HDAC2, HDAC4 and HDAC6, with significant degradation effects observed as early as 6 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:multiple myeloma MM.1S cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Reduced HDAC1 protein levels by 71%.
Achieved significant reduction of HDAC6 protein levels in MM.1S cells.\nInduced hyperacetylation of α-tubulin (a marker of HDAC6 inhibition) in MM.1S cells.
Induced hyperacetylation of histone H3 (a marker of class I HDAC inhibition) in MM.1S cells, with histone H3 hyperacetylation more pronounced than seen with comparator compounds.
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Cell Line:glioblastoma U-87MG cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Achieved significant degradation of HDAC1 and HDAC6 in U-87MG cells, though degradation was weaker than observed in MM.1S cells.
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Cell Line:multiple myeloma MM.1S cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Induced an increase in the sub G1 phase and a decrease in the S phase of the cell cycle, indicating cell cycle arrest.
Induced significant levels of early and late apoptosis, comparable to HDAC inhibitors.
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Cell Line:multiple myeloma MM.1S cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Induced significant apoptosis in MM.1S cells.
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Cell Line:MDA-MB-231 cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Reduced clonogenic growth of MDA-MB-231 cells, outperforming HDAC inhibitors Ricolinostat (HY-16026) and Vorinostat (HY-10221).
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Masse moléculaire 845.29
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Formule C43H56Cl3N5O6
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SMILES
O=C(NCCCCCCC(NO)=O)C1=CC=C(NC(CCCCCCCCCCCN(C(C2=CC=C(Cl)C(Cl)=C2)C(NCC3=CC=CC=C3)=O)C(CCl)=O)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FF2039 Related Classifications
HY-172159 Related Classifications
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