PROTAC HDAC6 degrader-13
PROTAC HDAC6 degrader-13 is a selective CRBN-recruiting HDAC6 PROTAC degrader. PROTAC HDAC6 degrader-13 does not affect class I HDACs. PROTAC HDAC6 degrader-13 inhibits TLR-NLRP3 inflammatory signaling. PROTAC HDAC6 degrader-13 is useful for research on acute myeloid leukemia.
(Pink: HDAC6 ligand (HY-189350); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Formula: C38H40ClN5O9
- Molecular Weight:746.21
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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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Biological Activity
Description
IC50 & Target
[1]|
HDAC6 |
Cereblon |
NLRP3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | IC50 |
36 μM
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Antiproliferative activity against human MM.1S multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 Cell Viability Assay.
Antiproliferative activity against human MM.1S multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo 2.0 Cell Viability Assay.
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42720482 |
In Vitro
PROTAC HDAC6 degrader-13 (Compound 9h) (0.2-1 μM; 25 h) potently degrades HDAC6 in HeLaHDAC6−HiBiT cells[1].
PROTAC HDAC6 degrader-13 exhibits potent concentration-dependent HDAC6 degradation in HeLaHDAC6−HiBiT cells with a Dmax50 of 17 nM[1].
PROTAC HDAC6 degrader-13-induced HDAC6 degradation in HeLaHDAC6−HiBiT cells requires CRBN, neddylation, and proteasome activity[1].
PROTAC HDAC6 degrader-13 (1 μM; 6 h) does not affect class I, class IIa HDACs, or HDAC8 in MM.1S cells[1].
PROTAC HDAC6 degrader-13 (72 h) exhibits weak antiproliferative activity against MM.1S cells[1].
PROTAC HDAC6 degrader-13 (0.1-10 μM; 24 h) does not strongly inhibit TLR4-mediated TNF secretion in THP-1 macrophages[1].
PROTAC HDAC6 degrader-13 (10 μM; 24 h) inhibits NLRP3 inflammasome-mediated IL-1β secretion in THP-1 macrophages[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
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Concentration:1 μM
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Incubation Time:6 h
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Result:Did not alter HDAC8 levels.
Did not affect HDAC1, HDAC2, and HDAC4 levels.
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Cell Line:THP-1 macrophages
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Concentration:0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Did not reduce TNF release at 0.1 and 1 μM.
At 10 μM, did not strongly inhibit TNF release.
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Cell Line:THP-1 macrophages
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Concentration:10 μM
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Incubation Time:24 h
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Result:Reduced IL-1β levels to a similar extent as ND-9h.
Chemical Information
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Molecular Weight 746.21
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Formula C38H40ClN5O9
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SMILES
O=C(N(CC(NCCCCCCCCOC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)CC4=CC=C(C(NO)=O)C=C4)C5=CC=CC=C5Cl
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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-13 Related Classifications
HY-189306 Related Classifications
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