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
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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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.
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Cell Line:A549 human lung cancer cells
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Concentration:1 μM, 10 μM
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Incubation Time:3 h, 6 h, 18 h, 24 h, 30 h, 48 h
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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.
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Cell Line:IMR-90 human lung fibroblasts
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Concentration:0.1 μM, 1 μM
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Incubation Time:18 h, 24 h
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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.
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Cell Line:TGF-β1-induced IMR-90 human lung fibroblasts
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Concentration:1 μM
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Incubation Time:48 h
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Result:Significantly reduced TGF-β1-induced fibronectin expression, which aligned with the reduction in HDAC6 levels.
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Cell Line:TGF-β1-induced IMR-90 human lung fibroblasts
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Concentration:1 μM
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Incubation Time:48 h
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Result:Disrupted the highly organized α-SMA stress fibers induced by TGF-β1, reducing their contractile fiber structure.
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Cell Line:A549 lung cancer cells
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Concentration:1 μM, 5 μM, 10 μM, 25 μM, 50 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Did not exhibit apparent cytotoxicity.
Chemical Information
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Molecular Weight 898.96
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Formula C47H50N10O9
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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
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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)
PROTAC HDAC6 degrader 5 Related Classifications
HY-174401 Related Classifications
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