PROTAC HDAC6 degrader 6
PROTAC HDAC6 degrader 6 is a HDAC6 PROTAC degrader that recruits CRBN, and also a photoactivatable photochemical targeting chimeric (PHOTAC). PROTAC HDAC6 degrader 6 switches between cis and trans conformations upon illumination, in which the cis conformation binds HDAC6 and CRBN to form a ternary complex, and induces HDAC6 degradation via ubiquitin-like modification, polyubiquitination and proteasomal pathways. PROTAC HDAC6 degrader 6 can be used in the research of multiple myeloma.
(Pink: Target protein ligand; Blue: Cereblon ligand (HY-A0003); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3068162-16-0
- Formula: C41H48N8O11
- Molecular Weight:828.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
HDAC6 |
In Vitro
When activated to the cis conformation by 390 nm light, PROTAC HDAC6 degrader 6 (PHOTAC 12) (1 μM; 6 h) induces approximately 50% HDAC6 degradation in MM.1S cells; in contrast, its trans conformation (protected from light, pre-irradiated with 505 nm light) causes less than 10% HDAC6 degradation[1].
PROTAC HDAC6 degrader 6 (1 μM; 6 h) selectively degrades HDAC6 but not HDAC1, HDAC3, or HDAC8 in MM.1S cells; its trans conformation does not degrade these off-target HDAC subtypes[1].
PROTAC HDAC6 degrader 6 (0.123-10 μM; 6 h) achieves maximum degradation of HDAC6 in MM.1S cells at 0.37 μM, and HDAC6 levels remain stable at concentrations up to 10 μM[1].
Degradation of HDAC6 in MM.1S cells mediated by PROTAC HDAC6 degrader 6 (1 μM; 6 h) depends on HDAC6 binding, CRBN recruitment, neddylation, and proteasomal activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S cells
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Concentration:1 μM
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Incubation Time:6 h
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Result:Selectively degraded HDAC6 over HDAC1, HDAC3, and HDAC8 in MM.1S cells when activated to its cis-state with 390 nm light, while its trans-state did not degrade these off-target HDAC isoforms.
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Cell Line:MM.1S cells
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Concentration:0.123, 0.37, 1.11, 3.33, 10 μM
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Incubation Time:6 h
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Result:Achieved maximum HDAC6 degradation in MM.1S cells at 0.37 μM, with stable HDAC6 levels at concentrations up to 10 μM.
Chemical Information
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CAS No. 3068162-16-0
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Molecular Weight 828.87
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Formula C41H48N8O11
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SMILES
COC(C=C1/N=N/C2=C3C(C(N(C4C(NC(CC4)=O)=O)C3)=O)=CC=C2)=C(C(OC)=C1)OCC(NCCCC(NC5=CC=C(C=C5)C(NCCCCCCC(NO)=O)=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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)