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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- CAS No.: 3100238-91-0
- Formule: C36H47N7O5
- Masse moléculaire:657.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
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
YL246 (compound A10) (1-16000 nM; 8 h) induces >95% HDAC8 degradation at 16 nM, with a DC50 of 3.75 nM in MDA-MB-231 cells, whereas no HDAC1/2/3 degradation is detected at concentrations up to 16 μM[1].
YL246 is metabolically unstable in CD-1 mouse liver microsomes, and its half-life is significantly shorter than that of the shorter ZBG analog[1].
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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CAS No. 3100238-91-0
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Masse moléculaire 657.80
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL246 Related Classifications
HY-189838 Related Classifications
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