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製品番号: 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).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3100238-91-0
分子式: C₃₆H₄₇N₇O₅
分子量:657.80

保管条件:

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

YL246 構造式

CAS 番号: 3100238-91-0

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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)

PROTACs アイソフォーム固有の製品をすべて表示 :

HDAC アイソフォーム固有の製品をすべて表示 :

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

体外実験

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

化学情報

CAS 番号 3100238-91-0
分子量 657.80
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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YL246

PROTACs アイソフォーム固有の製品をすべて表示

HDAC アイソフォーム固有の製品をすべて表示