1. PROTAC Metabolic Enzyme/Protease
  2. PROTACs SGK
  3. PROTAC SGK3 degrader-1

PROTAC SGK3 degrader-1  (Synonyms: SGK3-PROTAC1)

Cat. No.: HY-125878 Purity: 99.02%
COA Handling Instructions

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindau ligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).

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

PROTAC SGK3 degrader-1 Chemical Structure

PROTAC SGK3 degrader-1 Chemical Structure

CAS No. : 2381320-35-8

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1 mg USD 580 In-stock
5 mg USD 1180 In-stock
10 mg USD 1880 In-stock
50 mg USD 6400 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindau ligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate)[1].

IC50 & Target

SGK3

 

In Vitro

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (0.3 μM, 4 weeks) in combination with GDC0941 inhibits cell growth in CAMA-1 or ZR-75-1 cells[1].
PROTAC SGK3 degrader-1 (0.1 μM, 48 h) reduces SGK3 levels by 65% without effecting SGK1, SGK2, or S6K1 in HEK293 cells[1].
PROTAC SGK3 degrader-1 (1-10 μM, 48 h) moderate reduces S6K1 levels in HEK293 cells[1].
PROTAC SGK3 degrader-1 ( >0.1 μM, 8 h) reduces NDRG1 phosphorylation in HEK293 cells, and induces degradation of SGK3, but not SGK1 or S6K in CAMA-1 and ZR-75-1cells [1].

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

Cell Viability Assay[1]

Cell Line: CAMA-1 or ZR-75-1 cells
Concentration: 0.3 μM
Incubation Time: 4 weeks
Result: Inhibited cell growth in combination with GDC0941.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.1 μM
Incubation Time: 48 h
Result: Reduced SGK3 levels by 65% without effecting SGK1, SGK2, or S6K1.
Molecular Weight

1157.38

Formula

C57H73FN10O11S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C=C(C=C1)C)S(=O)(NC2=CC=C(C=C2)C3=NC4=C(C(OC[C@H]5CN(CCO5)CCCCCCOCCOCCOCC(N[C@H](C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)C(C)(C)C)=O)=N3)C=NN4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (86.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8640 mL 4.3201 mL 8.6402 mL
5 mM 0.1728 mL 0.8640 mL 1.7280 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.02%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8640 mL 4.3201 mL 8.6402 mL 21.6005 mL
5 mM 0.1728 mL 0.8640 mL 1.7280 mL 4.3201 mL
10 mM 0.0864 mL 0.4320 mL 0.8640 mL 2.1601 mL
15 mM 0.0576 mL 0.2880 mL 0.5760 mL 1.4400 mL
20 mM 0.0432 mL 0.2160 mL 0.4320 mL 1.0800 mL
25 mM 0.0346 mL 0.1728 mL 0.3456 mL 0.8640 mL
30 mM 0.0288 mL 0.1440 mL 0.2880 mL 0.7200 mL
40 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5400 mL
50 mM 0.0173 mL 0.0864 mL 0.1728 mL 0.4320 mL
60 mM 0.0144 mL 0.0720 mL 0.1440 mL 0.3600 mL
80 mM 0.0108 mL 0.0540 mL 0.1080 mL 0.2700 mL
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PROTAC SGK3 degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PROTAC SGK3 degrader-1
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