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).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C33H32AuCl2N7O6
- Masse moléculaire:890.52
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Stockage:
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]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
MERTK |
TXNL1 |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
58.5 μM
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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.
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41486557 |
In Vitro
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.
Chemical Information
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Masse moléculaire 890.52
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Formule C33H32AuCl2N7O6
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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
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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)
AuPROTAC Related Classifications
HY-188382 Related Classifications
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