PROTAC HDAC6 degrader 4
PROTAC HDAC6 degrader 4 is a potent and selective HDAC6 PROTAC degrader with an IC50 of 0.295 μM. PROTAC HDAC6 degrader 4 bridges HDAC6 and the CRBN E3 ubiquitin ligase to form a ternary complex, thereby inducing the specific degradation of HDAC6 via the ubiquitin-proteasome system. PROTAC HDAC6 degrader 4 can be used in studies related to multiple myeloma.
(Pink: HDAC6 ligand (HY-172360); Blue: Cereblon ligand (HY-W093272); Black: linker (HY-138387)).
For research use only. We do not sell to patients.
- Formula: C39H42FN9O7
- Molecular Weight:767.81
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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
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Biological Activity
Description
IC50 & Target
[1]|
HDAC6 14 nM (DC50) |
HDAC6 0.295 μM (IC50) |
HDAC3 0.611 μM (IC50) |
HDAC1 2.20 μM (IC50) |
HDAC2 2.37 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM.1S | IC50 |
>50.0 μM
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Reduction of multiple myeloma MM.1S cell viability assessed by CellTiter-Glo assay.
Reduction of multiple myeloma MM.1S cell viability assessed by CellTiter-Glo assay.
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40104802 |
| MM.1S | DC50 |
14 nM
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Half-maximal degradation of HDAC6 protein in multiple myeloma MM.1S cells incubated for 24 hrs, measured by automated capillary Western blot assay.
Half-maximal degradation of HDAC6 protein in multiple myeloma MM.1S cells incubated for 24 hrs, measured by automated capillary Western blot assay.
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40104802 |
In Vitro
PROTAC HDAC6 degrader 4 (Compound 17c) (pre-incubated at room temperature for 1 h) exhibits inhibitory effects on purified HDAC1, HDAC2, HDAC3 and HDAC6 proteins in cell-free biochemical assays, with corresponding IC50 values of 2.20 μM, 2.37 μM, 0.611 μM and 0.295 μM[1].
PROTAC HDAC6 degrader 4 (up to 50 μM) exhibits extremely weak inhibitory effects on the viability of multiple myeloma MM.1S cells, with an IC50 >50.0 μM[1].
PROTAC HDAC6 degrader 4 (0.05 nM-5 μM; 6-24 h) induces dose-dependent and selective degradation of HDAC6, but not HDAC1-3, in MM.1S cells, with a DC50 of 14 nM. It promotes hyperacetylation of the HDAC6 substrate α-tubulin without affecting HDAC1 levels, and simultaneously induces the degradation of IKZF3 and MIER1[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:0.05 nM, 0.5 nM, 5 nM, 0.05 μM, 0.5 μM, 5 μM
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Incubation Time:24 h
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Result:Significantly degraded HDAC6, increased the acetylation level of the substrate α-tubulin, and did not degrade HDAC1, HDAC2, and HDAC3.
Exhibited a half-maximal degradation concentration (DC50) of 14 nM for HDAC6 in MM.1S cells.
Chemical Information
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Molecular Weight 767.81
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Formula C39H42FN9O7
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SMILES
O=C(NCC1=CC=C(C(NNCC)=O)C=C1)C2=CC=C(OCC3=CN(CCCCCCNC4=CC5=C(C(N(C(CC6)C(NC6=O)=O)C5=O)=O)C=C4F)N=N3)C=C2
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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 4 Related Classifications
HY-172359 Related Classifications
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