2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs HDAC Ligands for E3 Ligase
  4. 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: Target protein ligand (HY-174408), Target protein ligand + linker (HY-174409); Blue: Pomalidomide (HY-10984), Pomalidomide 4'-alkylC3-azide (HY-139341)).

For research use only. We do not sell to patients.

PROTAC HDAC6 degrader 5 Chemical Structure

PROTAC HDAC6 degrader 5 Chemical Structure

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PROTAC HDAC6 degrader 5 Related Antibodies

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Description

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: Target protein ligand (HY-174408), Target protein ligand + linker (HY-174409); Blue: Pomalidomide (HY-10984), Pomalidomide 4'-alkylC3-azide (HY-139341))[1].

IC50 & Target

hHDAC1

162 nM (IC50)

hHDAC8

864 nM (IC50)

hHDAC10

2447 nM (IC50)

In Vitro

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.

PROTAC HDAC6 degrader 5 Related Antibodies

Immunofluorescence[1]

Cell Line: IMR-90 cells (TGF-β1-induced fibrosis model)
Concentration: 1 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: A549 cells, IMR-90 cells, IMR-90 cells (TGF-β1-induced fibrosis model)
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 3 h, 6 h, 18 h, 24 h, 30 h, 48 h
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.
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.
Purity & Documentation
References
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PROTAC HDAC6 degrader 5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC HDAC6 degrader 5PROTACsHDACLigands for E3 LigaseHistone deacetylasesE3 ligase-recruiting MoietyIdiopathic Pulmonary Fibrosis (IPF)TGF-β1-induced fibrosisA549 cellsIMR-90 cellsHDAC6CRBNPROTACInhibitorinhibitorinhibit

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