PROTAC HDAC6 degrader 5
PROTAC HDAC6 degrader 5 (Compound 5a) is a highly selective PROTAC targeting HDAC6. PROTAC HDAC6 degrader 5 can effectively degrade HDAC6 in cells (IC50 = 43 nM). PROTAC HDAC6 degrader 5 reduces HDAC6 levels through proteasome- and CRBN-dependent mechanisms.
(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
All PROTACs Isoforms
More
Biological Activity
|
hHDAC1 162 nM (IC50) |
hHDAC8 864 nM (IC50) |
hHDAC10 2447 nM (IC50) |
PROTAC HDAC6 degrader 5 (Compound 5a) (1 μM, 48 h) disrupts TGF-β1-induced α-SMA fiber structure and reverses myofibroblast differentiation in IMR-90 cells[1].
PROTAC HDAC6 degrader 5 (1 μM, 10 μM, 3-48 h) Significantly reduces HDAC6 protein levels in IMR-90 cells[1].
PROTAC HDAC6 degrader 5 (0.1 μM, 1 μM, 24 h) effectively degrades HDAC6 and restores α-tubulin acetylation in IMR-90 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IMR-90 cells (TGF-β1-induced fibrosis model)
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Concentration:1 μM
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Incubation Time:48 h
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Result:Disrupted the fibers, rendering them less organized.
Reduced and reversed the inhibitory effects on HDAC6 when co-treated with MG-132, and restored TGF-β1-induced fibronectin expression.
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Cell Line:A549 cells, IMR-90 cells, IMR-90 cells (TGF-β1-induced fibrosis model)
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Concentration:0.1 μM, 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:Had a good degradation effect on HDAC6 at 10 μM, and the degradation reached peaks at 6 and 18 hours in A549 cells.
Reduced the expression of sirtuins significantly and caused a statistically significant increase in the content of acetylated α-tubulin.
Induced maximal degradation of HDAC6 at 1 μM after 24 h of treatment, whereas no decrease in the expression of HDAC1 was observed.
Selectively degraded HDAC6 via the CRBN-proteasome pathway, and the neddylation-independent CRL4 complex was not activated.
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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