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Art. -Nr.: HY-189838

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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. Nr.: 3100238-91-0
Formel: C₃₆H₄₇N₇O₅
Molecular Weight:657.80

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

YL246 Chemical Structure

CAS. Nr.: 3100238-91-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: HDAC8 ligand (HY-163846); Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target

^[1]

HDAC8

3.75 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	DC₅₀	3.75 nM	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.	acs.jmedchem.6c01636

In Vitro

Protein/Amino Acid MetabolismOthers

Protein/Amino Acid Metabolism

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].

Others

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.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 human breast cancer cells
Concentration:

1, 4, 16, 64, 250, 1000, 4000, 16000 nM
Incubation Time:

8 h
Result:

Observed dose‑dependent HDAC8 degradation starting at 4 nM, with DC₅₀ = 3.75 nM and D_max = 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.

Related Protocols :

Breast Cancer Modeling

Chemical Information

CAS. Nr. 3100238-91-0
Molecular Weight 657.80
Formel C₃₆H₄₇N₇O₅
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Liu Y, et al. A 2‑in‑1 Strategy for the Discovery of Compact HDAC8 Protac Degraders. Journal of Medicinal Chemistry. 2026;69(18):21381‑21397.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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YL246

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle HDAC Isoform-spezifische Produkte anzeigen