AuPROTAC
AuPROTAC is a dual MERTK and TXNL1 PROTAC degrader containing a cyclometalated Au (III) complex. AuPROTAC specifically covalently binds the target proteins MERTK and TXNL1 through a gold-template-based two-step mechanism (gold-thiol coordination and cysteine arylation), while recruiting the CRBN E3 ubiquitin ligase to form a ternary complex, mediating the ubiquitination and degradation of MERTK and TXNL1. AuPROTAC can be used for research on acute myeloid leukemia.
(Pink: TXNL1 and MERTK ligand (HY-188383); Blue: Cereblon ligand (HY-14658); 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。
- 分子式: C33H32AuCl2N7O6
- 分子量:890.52
-
保管条件:
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
MERTK |
TXNL1 |
Cereblon |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
58.5 μM
|
Cytotoxicity against PMA-differentiated HL-60 cells assessed as viability reduction incubated 24 hrs by dose-response assay.
Cytotoxicity against PMA-differentiated HL-60 cells assessed as viability reduction incubated 24 hrs by dose-response assay.
|
41486557 |
体外実験
AuPROTAC (8 h) reduces the viability of PMA-differentiated HL-60 cells in the presence of CHX (HY-12320), with an IC50 of 64.3 µM[1].
AuPROTAC (60 μM; 0.5-8 h) combined with 10 μM CHX quantitatively degrades MERTK and TXNL1 and partially degrades SLC3A2 and NOTCH2 in PMA-differentiated HL-60 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
分子量 890.52
-
分子式 C33H32AuCl2N7O6
-
SMILES
O=C1C(CCC(N1)=O)N2C(C3=C(C(N4CCN(CCNC(CO/N=C5C6=CC=CC=[C-]6[Au+3]([Cl-])([Cl-])[N]7=C/5C=CC=C7)=O)CC4)=CC=C3)C2=O)=O
-
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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AuPROTAC 関連分類
HY-188382 関連分類
Powered by Bioz