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PROTAC SGK3 degrader-1

Synonyms: SGK3-PROTAC1

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.

PROTAC SGK3 degrader-1 Chemical Structure

PROTAC SGK3 degrader-1 Chemical Structure

CAS No. 2381320-35-8

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PROTAC SGK3 degrader-1 Related Products

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
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]
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 1157.38 Formula

C57H73FN10O11S2
CAS No. 2381320-35-8 SDF --
Smiles CC1=CC=C(F)C(=C1)[S](=O)(=O)NC2=CC=C(C=C2)C3=NC4=C(C=N[NH]4)C(=N3)OCC5CN(CCCCCCOCCOCCOCC(=O)NC(C(=O)N6CC(O)CC6C(=O)NCC7=CC=C(C=C7)C8=C(C)N=CS8)C(C)(C)C)CCO5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (86.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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