YL246
YL246 is a selective, CRBN-recruiting HDAC8 PROTAC degrader, DC50 = 3.75 nM. YL246 induces CRBN- and proteasome-dependent degradation of zinc-dependent HDAC8 through CRBN ligand-mediated ubiquitination. YL246 has poor metabolic stability. YL246 can be used for HDAC8-mediated cancer-related research, such as breast cancer.
(Pink: HDAC8 ligand (HY-163846); Blue: Cereblon ligand (HY-41547); Black: linker).
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- No. CAS: 3100238-91-0
- Fòrmula: C36H47N7O5
- Peso molecular:657.80
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC8 3.75 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | DC50 |
3.75 nM
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Half-maximal degradation concentration of HDAC8 in human MDA-MB-231 breast cancer cells after 8 hrs incubation by Western blot analysis.
Half-maximal degradation concentration of HDAC8 in human MDA-MB-231 breast cancer cells after 8 hrs incubation by Western blot analysis.
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acs.jmedchem.6c01636 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:1, 4, 16, 64, 250, 1000, 4000, 16000 nM
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Incubation Time:8 h
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Result:Observed dose‑dependent HDAC8 degradation starting at 4 nM, with DC50 = 3.75 nM and Dmax = 87%.
Detected no measurable degradation of HDAC3, HDAC1, or HDAC2 at concentrations up to 16 μM.
Confirmed that HDAC8 degradation was CRBN‑ and proteasome‑dependent.
Chemical Information
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No. CAS 3100238-91-0
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Peso molecular 657.80
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Fòrmula C36H47N7O5
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SMILES
O=C(NNCCCCCC)C(C=C1)=CC=C1N(CC2)CCN2CC3CCN(C4=C(C5=O)C(C(N5C(C(N6)=O)CCC6=O)=O)=CC=C4)CC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL246 Related Classifications
HY-189838 Related Classifications
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