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Cat. No.: HY-184524

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC HDAC4 Degrader-2 Chemical Structure

CAS No.: 3035189-46-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

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^[1]. (Pink: HDAC4 ligand (HY-W039803); Blue: VHL ligand (HY-125845); Black: linker (HY-184526)).

IC₅₀ & Target^[1]

HDAC4

0.15 μM (IC₅₀)

All PROTACs Isoforms :

All HDAC Isoforms :

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.

Chemical Information

CAS No. 3035189-46-6
Molecular Weight 1075.24
Formula C₅₂H₇₃F₃N₈O₁₁S
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
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

Handling Instructions (2659 KB)

References

[1]. Macabuag N, Esmieu W, Breccia P, et al.. Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology. Journal of medicinal chemistry. 2022 Sep 22;65(18):12445-12459. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC HDAC4 Degrader-2

All PROTACs Isoforms

All HDAC Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC HDAC4 Degrader-2 Related Classifications

HY-184524 Related Classifications