PROTAC HDAC4 Degrader-2
PROTAC HDAC4 Degrader-2 is a class IIa selective negative control for HDAC4 PROTAC degraders, with an IC50 of 0.15 μM against HDAC4 and a cellular IC50 of 0.18 μM. PROTAC HDAC4 Degrader-2 fails to effectively recruit the VHL E3 ligase, and thus does not induce significant degradation of HDAC4 protein.
(Pink: HDAC4 ligand (HY-W039803); Blue: VHL ligand (HY-125845); Black: linker (HY-184526)).
For research use only. We do not sell to patients.
- CAS No.: 3035189-46-6
- Formula: C52H73F3N8O11S
- Molecular Weight:1075.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
HDAC4 0.15 μM (IC50) |
In Vitro
PROTAC HDAC4 Degrader-2 (Compound 12) inhibits recombinant HDAC4 catalytic activity with an IC50 of 0.15 μM[1].
PROTAC HDAC4 Degrader-2 (24 h) inhibits cellular class IIa HDAC activity in Jurkat E6-1 cells with an IC50 of 0.18 μM and is selective over class I HDACs[1].
PROTAC HDAC4 Degrader-2 (0.05 nM-10 μM; 24 h) does not significantly degrade HDAC4 in Jurkat E6-1 cells, with a DC50 >10,000 nM and only 50% maximum degradation at 10 μM[1].
PROTAC HDAC4 Degrader-2 (0.05 nM-10 μM; 24 h) fails to induce HDAC4 degradation in Jurkat E6-1 cells across concentrations ranging from 0.05 nM to 10 μM after 24 hours of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3035189-46-6
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Molecular Weight 1075.24
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Formula C52H73F3N8O11S
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SMILES
O=C(C1=CC=C(C2=NOC(C(F)(F)F)=N2)C=C1)N[C@H](C)CN(CCC)CCCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)=O)=O
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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.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC HDAC4 Degrader-2 Related Classifications
HY-184524 Related Classifications
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