PROTAC SGK3 degrader-1

Catalog No.S9672 Batch:S967201

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Technical Data

Formula

C57H73FN10O11S2
Molecular Weight 1157.38 CAS No. 2381320-35-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (86.4 mM)
Ethanol 100 mg/mL (86.4 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation.
Targets
SGK3 [1]
In vitro

SGK3-PROTAC1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 h, with maximal 80% degradation observed within 8 h, accompanied by a loss of phosphorylation of NDRG1, an SGK3 substrate. Low doses of SGK3-PROTAC1 (0.1−0.3 μM) restores sensitivity of SGK3 dependent ZR-75-1 and CAMA-1 breast cancer cells to Akt and PI3K inhibitors, whereas the cis epimer analogue incapable of binding to the VHL E3 ligase has no impact. SGK3-PROTAC1 suppresses proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor more effectively than could be achieved by a conventional SGK isoform inhibitor.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    CAMA-1, HEK293 cells

  • Concentrations

    0.3 μM

  • Incubation Time

    8 h

  • Method

    Cells are treated with DMSO (control), SGK3-PROTAC1 (0.3 μM), or cisSGK3-PROTAC1 (0.3 μM) for 8 h and lysed. Lysates are subjected to immunoblot analysis with the indicated antibodies.

Selleck's PROTAC SGK3 degrader-1 has been cited by 2 publications

The role of the SGK3/TOPK signaling pathway in the transition from acute kidney injury to chronic kidney disease [ Front Pharmacol, 2023, 14:1169054] PubMed: 37361201
The role of the SGK3/TOPK signaling pathway in the transition from acute kidney injury to chronic kidney disease [ Front Pharmacol, 2023, 14:1169054] PubMed: 37361201

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.