FF2049
FF2049 is a selective HDAC1-3 PROTAC degrader (with a DC50 of 257 nM against HDAC1). FF2049 recruits the E3 ligase FEM1B to mediate ubiquitination and proteasomal degradation of HDAC1-3. FF2049 induces cell cycle arrest and Apoptosis in cells. FF2049 can be used in research related to multiple myeloma, acute monocytic leukemia, triple-negative breast cancer and glioblastoma.
(Pink: HDAC ligand (HY-168864); Blue: FEM1B ligand (HY-168865); Black: linker (HY-Y0966)).
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- 分子式: C31H38ClN7O7
- 分子量:656.13
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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HDAC1 257 nM (DC50) |
HDAC2 |
HDAC3 |
FF2049 (90 min) potently inhibits recombinant HDAC1, HDAC2 and HDAC6 enzymes, with IC50 values of 0.074 μM, 0.156 μM and 0.009 μM, respectively; it shows weak inhibitory activity against HDAC4, with an IC50 of 13.3 μM[1].
FF2049 (2.5-25000 nM; 24 h) induces potent, concentration-dependent HDAC1 degradation in MM.1S cells via a FEM1B-, HDAC1- and neddylation-dependent mechanism, with a DC50 of 257 nM and a D_max of 85.2%, while leaving HDAC6 levels unaffected[1].
FF2049 (1 μM; 24 h) selectively degrades HDAC1, HDAC2 and HDAC3 in MM.1S cells without affecting other tested HDAC isoforms; it also exhibits strong cellular target-binding capacity, as evidenced by increased hyperacetylation levels of histone H3 and α-tubulin[1].
FF2049 (0.5 μM; 6 h) significantly induces the degradation of HDAC1 and HDAC2 in MM.1S cells, accompanied by the degradation of associated multi-subunit complex proteins (KDM1A, RCOR1, RCOR3, SIN3A, NCOR1, MIER1)[1].
FF2049 (10 μM; 24 h) induces significant HDAC1 degradation in MV4-11 (87%), MDA-MB-231 (53%) and U-87MG (75%) cells, confirming its activity against various cancer cell types[1].
FF2049 (71-72 h) exhibits antiproliferative activity against MM.1S (EC50 2.33 μM), MV4-11 (EC50 0.958 μM), MDA-MB-231 (EC50 26.5 μM) and U-87MG (EC50 37.4 μM) cells[1].
FF2049 (10 μM; 48 h) induces cell cycle arrest and apoptosis in MM.1S cells, which is evidenced by the decreased proportion of cells in S phase and increased proportion of cells in sub-G1 phase after treatment with 10 μM FF2049 for 48 h[1].
FF2049 (10 μM; 48 h) significantly induces early and late apoptosis in MM.1S cells after treatment at 10 μM for 48 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human multiple myeloma MM.1S cells
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Concentration:2.5-25000 nM (24 h incubation); 1 μM (24 h incubation); 1 μM (6 h incubation with pre-treatment)
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Incubation Time:24 h; 6 h (with 30 min pre-incubation for co-treatment groups)
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Result:Induced concentration-dependent HDAC1 degradation with a half-maximal degradation concentration (DC50) of 257 nM and a maximal degradation (D_max) of 85.2% after 24 h treatment.
Induced 62.3% degradation of HDAC1 at 1 μM for 24 h, while HDAC6 levels remained largely unaffected.
Blocked HDAC1 degradation by co-treatment with the non-degrading control 1g-nc, the neddylation inhibitor MLN4924, or the HDAC inhibitor vorinostat.
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Cell Line:human multiple myeloma MM.1S cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced strong degradation of HDAC1, HDAC2, and HDAC3, while HDAC4, HDAC6, and HDAC8 levels remained unaffected.
Increased hyperacetylation of histone H3 (a marker of class I HDAC inhibition/degradation) and α-tubulin (a marker of HDAC6 inhibition) compared to vehicle control.
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Cell Line:human acute monocytic leukemia MV4-11 cells, human triple-negative breast cancer MDA-MB-231 cells, human glioblastoma U-87MG cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced 87% HDAC1 degradation in MV4-11 cells.
Induced 53% HDAC1 degradation in MDA-MB-231 cells.
Induced 75% HDAC1 degradation in U-87MG cells.
The non-degrading control 1g-nc did not affect HDAC1 levels in any cell line.
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Cell Line:human multiple myeloma MM.1S cells, human acute monocytic leukemia MV4-11 cells, human triple-negative breast cancer MDA-MB-231 cells, human glioblastoma U-87MG cells
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Concentration:Increasing concentrations
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Incubation Time:72 h (MM.1S, MV4-11); 71 h (MDA-MB-231, U-87MG)
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Result:Exhibited antiproliferative activity with an EC50 of 2.33 μM in MM.1S cells.
Exhibited antiproliferative activity with an EC50 of 0.958 μM in MV4-11 cells.
Exhibited antiproliferative activity with an EC50 of 26.5 μM in MDA-MB-231 cells.
Exhibited antiproliferative activity with an EC50 of 37.4 μM in U-87MG cells.
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Cell Line:human 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 a significant increase in both early and late apoptotic cell populations compared to vehicle control.
化学情報
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分子量 656.13
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分子式 C31H38ClN7O7
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SMILES
ONC(CCCCCCNC(C1=CC=C(C=C1)NC(CNC(CN2CCOC3=C2C=CC(N(C(CCl)=O)CCC#N)=C3)=O)=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Feller F, et al. Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders. Journal of medicinal chemistry. 2025 Jan 23;68(2):1824-1843. [Content Brief]
[2]. Hanl M, et al. Target Engagement Studies and Kinetic Live-Cell Degradation Assays Enable the Systematic Characterization of Histone Deacetylase 6 Degraders. ACS pharmacology & translational science. 2025 Sep 12;8(9):3074-3089. [Content Brief]
Calculators
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FF2049 関連分類
HY-168863 関連分類
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