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

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

製品番号: HY-125878 純度: 99.89%
COA 取扱説明書 Technical Support

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), a chemical probe, is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate).

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PROTAC SGK3 degrader-1

PROTAC SGK3 degrader-1 構造式

CAS 番号 : 2381320-35-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1909 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1909 在庫あり
Solid
1 mg $300 在庫あり
5 mg $885 在庫あり
10 mg $1500 在庫あり
25 mg $2700 在庫あり
50 mg $4320 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 5 publication(s) in Google Scholar

PROTAC SGK3 degrader-1 関連抗体

Top Publications Citing Use of Products

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

SGK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
SGK1 SGK3 SGK2

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

PROTAC SGK3 degrader-1 (SGK3-PROTAC1), a chemical probe, is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate)[1].

IC50 & Target[1]

VHL

 

SGK3

 

体外実験

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.

PROTAC SGK3 degrader-1 関連抗体

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.
分子量

1157.38

分子式

C57H73FN10O11S2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

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

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
10 mM 0.0864 mL 0.4320 mL 0.8640 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
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
純度とドキュメンテーション

純度: 99.89%

COA (245 KB) HNMR (362 KB) RP-HPLC (268 KB) LCMS (91 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

PROTAC SGK3 degrader-12381320-35-8SGK3-PROTAC1PROTACsSGKSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseInhibitorinhibitorinhibit

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製品名:
PROTAC SGK3 degrader-1
製品番号:
HY-125878
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