PROTAC HDAC6 degrader 5
PROTAC HDAC6 degrader 5 is a selective HDAC6 PROTAC degrader with an IC50 of 43 nM. PROTAC HDAC6 degrader 5 induces proteasome-dependent degradation of HDAC6 by bridging HDAC6 and CRBN to form a ternary complex. PROTAC HDAC6 degrader 5 is applicable to research related to pulmonary fibrosis.
(Pink: HDAC ligand (HY-174408); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Formula: C47H50N10O9
- Molecular Weight:898.96
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
hHDAC6 43 nM (IC50) |
hHDAC1 462 nM (IC50) |
hHDAC8 864 nM (IC50) |
hHDAC10 2447 nM (IC50) |
α-Tubulin |
In Vitro
PROTAC HDAC6 degrader 5 (Compound 5a) (1-50 μM; 3-72 h) shows no obvious cytotoxicity in A549 and IMR-90 cells, significantly degrades HDAC6 and increases the acetylation level of α-tubulin, and exerts the effect of selectively degrading HDAC6 without affecting HDAC1 protein expression in IMR-90 cells[1].
PROTAC HDAC6 degrader 5 (1 μM; 48 h) significantly reduces the expression of the profibrotic marker fibronectin in TGF-β1 (HY-P78213)-induced IMR-90 cells, which is consistent with the decrease in HDAC6 levels, and disrupts highly assembled α-SMA stress fibers[1].
PROTAC HDAC6 degrader 5 selectively inhibits the activity of HDAC6 in in vitro enzymatic inhibition assays, with an IC50 of 43 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:A549 human lung cancer cells
-
Concentration:1 μM, 10 μM
-
Incubation Time:3 h, 6 h, 18 h, 24 h, 30 h, 48 h
-
Result:Reduced HDAC6 levels and increased acetylated α-tubulin levels at 10 μM for 24 h.
Achieved peak HDAC6 degradation at 6 h and 18 h at 10 μM, with strong α-tubulin acetylation observed at 3 h, 30 h, and 48 h.
Showed no significant HDAC6 degradation across all time points at 1 μM, with marked α-tubulin acetylation only at 48 h.
-
Cell Line:IMR-90 human lung fibroblasts
-
Concentration:0.1 μM, 1 μM
-
Incubation Time:18 h, 24 h
-
Result:Significantly reduced HDAC6 levels and caused a marked increase in acetylated α-tubulin levels at 1 μM for 24 h.
Showed no significant HDAC6 degradation at 0.1 μM (18 h or 24 h) or at 1 μM for 18 h.
-
Cell Line:TGF-β1-induced IMR-90 human lung fibroblasts
-
Concentration:1 μM
-
Incubation Time:48 h
-
Result:Significantly reduced TGF-β1-induced fibronectin expression, which aligned with the reduction in HDAC6 levels.
-
Cell Line:TGF-β1-induced IMR-90 human lung fibroblasts
-
Concentration:1 μM
-
Incubation Time:48 h
-
Result:Disrupted the highly organized α-SMA stress fibers induced by TGF-β1, reducing their contractile fiber structure.
-
Cell Line:A549 lung cancer cells
-
Concentration:1 μM, 5 μM, 10 μM, 25 μM, 50 μM
-
Incubation Time:24 h, 48 h, 72 h
-
Result:Did not exhibit apparent cytotoxicity.
Chemical Information
-
Molecular Weight 898.96
-
Formula C47H50N10O9
-
SMILES
O=C(NO)C1=CC=C(CN2C(C3=CC=CN=C3)C(C)(C)C4=C2C=CC(NC(CCCOCC5=CN(CCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)N=N5)=O)=C4)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
-
Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)