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Cat. No.: HY-D2336

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PROTAC Aster-A degrader-1

PROTAC Aster-A degrader-1 is a PROTAC degrader targeting the sterol transporter (Aster-A), with a DC₅₀ of 4.8 μM. PROTAC Aster-A degrader-1 binds to the sterol-binding domain of Aster-A, with a FI-K_d value of 83 nM. PROTAC Aster-A degrader-1 induces CRL- and proteasome-dependent degradation of Aster-A and inhibits autophagy in cancer cells. PROTAC Aster-A degrader-1 serves as a fluorescent probe. PROTAC Aster-A degrader-1 is useful for research related to cervical cancer, breast cancer, and lung adenocarcinoma.
(Pink: ligand (HY-128340); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W442085)).

For research use only. We do not sell to patients.

CAS No.: 3038774-43-2
Formula: C₄₂H₅₁N₇O₁₀S
Molecular Weight:845.96

Storage:

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

Data Sheet (272 KB)

PROTAC Aster-A degrader-1 Chemical Structure

CAS No.: 3038774-43-2

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

PROTAC Aster-A degrader-1 is a PROTAC degrader targeting the sterol transporter (Aster-A), with a DC₅₀ of 4.8 μM. PROTAC Aster-A degrader-1 binds to the sterol-binding domain of Aster-A, with a FI-K_d value of 83 nM. PROTAC Aster-A degrader-1 induces CRL- and proteasome-dependent degradation of Aster-A and inhibits autophagy in cancer cells. PROTAC Aster-A degrader-1 serves as a fluorescent probe. PROTAC Aster-A degrader-1 is useful for research related to cervical cancer, breast cancer, and lung adenocarcinoma^[1]. (Pink: ligand (HY-128340); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W442085)).

IC₅₀ & Target

^[1]

Aster-A

4.8 μM (DC₅₀)

All PROTACs Isoforms :

In Vitro

Anti-cancerAutophagyOthers

Anti-cancer

PROTAC Aster-A degrader-1 (10 µM; 1 h) is cell-permeable, as shown by fluorescence in HeLa cells^[1].
PROTAC Aster-A degrader-1 (0-20 µM; 18 hours) degrades Aster-A in HeLa cells with a DC₅₀ of 4.8 µM and a D_max of 60%^[1].
PROTAC Aster-A degrader-1 does not degrade Aster-A in A549 or MCF7-eGFP-LC3 cells, indicating that its activity is cell line-dependent^[1].

Anti-cancer

Autophagy

PROTAC Aster-A degrader-1 (3 µM) inhibits autophagy in MCF7-eGFP-LC3 cells^[1].

Others

PROTAC Aster-A degrader-1 serves as a turn-on fluorescent probe for Aster-A, with a FI-K_d value of 83 nM^[1].
PROTAC Aster-A degrader-1 binds tightly to Aster-A with a K_d of 90 nM, as determined by FP assay^[1].
PROTAC Aster-A degrader-1 is suitable as a fluorescent probe in biophysical assays, with an optimal concentration of 100 nM for competitive assays^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence^[1]

Cell Line:

HeLa cells
Concentration:

10 µM
Incubation Time:

1 h
Result:

Showed intracellular fluorescence.

Western Blot Analysis^[1]

Cell Line:

HeLa cells
Concentration:

0, 1.3, 2.5, 5, 10 and 20 µM
Incubation Time:

18 h
Result:

Degraded Aster-A in a dose-dependent manner, with an approximate reduction of 50% at 10 µM, a DC₅₀ of 4.8 µM, and a Dmax of 60%.

Related Protocols :

Chemical Information

CAS No. 3038774-43-2
Molecular Weight 845.96
Formula C₄₂H₅₁N₇O₁₀S
SMILES

O=C(NC1=NC2=C(CN(C(OC(C)(C)C)=O)CC2)S1)C3=CC=C(C(NCCCOCCCCOCCCNC4=CC=CC5=C4C(N(C6CCC(NC6=O)=O)C5=O)=O)=O)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. He N, et al. Fluorescent probes and degraders of the sterol transport protein Aster-A. Bioorganic & medicinal chemistry. 2024 Apr 01;103:117673. [Content Brief]

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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.

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