| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
PROTAC SGK3 degrader-1 targets SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3). It is a heterobifunctional molecule that binds to SGK3 and recruits the VHL E3 ubiquitin ligase. This leads to the ubiquitination and proteasomal degradation of SGK3.
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|---|---|
| ln Vitro |
When coupled with GDC0941, PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (0.3 μM, 4 weeks) suppresses the development of CAMA-1 or ZR-75-1 cells [1]. Within HEK293 cells, PROTAC SGK3 degrader-1 (0.1 μM, 48 h) 2 decreases SGK3 levels by 65% while leaving SGK1, SGK2, and S6K1 expression levels unchanged [1]. In HEK293 cells, PROTAC SGK3 degrader-1 (1–10 μM, 48 h) regulates the decrease in S6K1 levels [1]. SGK3 degrader-1 (>0.1 μM, 8 h) can promote SGK3 phosphorylation in CAMA-1 and ZR-75-1 cells and diminish NDRG1 phosphorylation in HEK293 cells, but not SGK1 or S6K phosphorylation [1].
In vitro, PROTAC SGK3 degrader-1 (0.1 μM, 48 h) decreases SGK3 levels by 65% in HEK293 cells while leaving SGK1, SGK2, and S6K1 expression unchanged. It (1–10 μM, 48 h) regulates the decrease in S6K1 levels. The compound inhibits GDC0941-induced proliferation of cancer cells. |
| ln Vivo |
In vivo activity data for PROTAC SGK3 degrader-1 are not extensively detailed in the available sources. The compound enables researchers to study SGK3 biology, downstream PI3K/AKT signaling, and its roles in cancer progression and resistance mechanisms.
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| Enzyme Assay |
The in vitro degradation assay for PROTAC SGK3 degrader-1 involves measuring the reduction in SGK3 protein levels. HEK293 cells are treated with the compound at concentrations of 0.1-10 μM for 48 hours. SGK3 protein levels are quantified by Western blotting.
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| Cell Assay |
Cell viability assay [1]
Cell Types: CAMA-1 or ZR-75-1 Cell Tested Concentrations: 0.3 μM Incubation Duration: 4 weeks Experimental Results: Cell growth can be inhibited when used in combination with GDC0941. Western Blot Analysis[1] Cell Types: HEK293 Cell Tested Concentrations: 0.1 μM Incubation Duration: 48 hrs (hours) Experimental Results: 65% reduction in SGK3 levels without affecting SGK1, SGK2 or S6K1. Cellular assays for PROTAC SGK3 degrader-1 are performed using HEK293 cells. Cells are treated with the compound at various concentrations. SGK3 degradation is assessed by Western blotting. The compound's effects on downstream signaling, such as NDRG1 phosphorylation, are also evaluated. |
| Animal Protocol |
In vivo animal studies for PROTAC SGK3 degrader-1 are not detailed in the available sources. The compound is a research tool for studying SGK3 function. Specific animal models, dosing regimens, and efficacy data have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PROTAC SGK3 degrader-1 are not available in the provided sources. The compound is a PROTAC molecule with a higher molecular weight. Specific PK parameters such as half-life, bioavailability, and clearance have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for PROTAC SGK3 degrader-1 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. Specific toxicological profiles have not been characterized.
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| References | |
| Additional Infomation |
PROTAC SGK3 degrader-1 is a research compound for studying SGK3 function in cancer and metabolism. It is a potent SGK3 degrader that induces degradation of endogenous SGK3. The compound is available from commercial suppliers for research purposes only.
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| Molecular Formula |
C57H73FN10O11S2
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|---|---|
| Molecular Weight |
1157.37833476067
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| Exact Mass |
1156.488
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| CAS # |
2381320-35-8
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| PubChem CID |
139035049
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| Appearance |
White to off-white solid powder
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| LogP |
6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
81
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| Complexity |
2050
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| Defined Atom Stereocenter Count |
4
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| SMILES |
S1C=NC(C)=C1C1C=CC(=CC=1)CNC([C@@H]1C[C@H](CN1C([C@H](C(C)(C)C)NC(COCCOCCOCCCCCCN1CCO[C@@H](COC2C3C=NNC=3N=C(C3C=CC(=CC=3)NS(C3C(=CC=C(C)C=3)F)(=O)=O)N=2)C1)=O)=O)O)=O
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| InChi Key |
RTFQFPZKDYMMMJ-RIAKQDHQSA-N
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| InChi Code |
InChI=1S/C57H73FN10O11S2/c1-37-10-19-46(58)48(28-37)81(73,74)66-42-17-15-41(16-18-42)52-63-53-45(31-61-65-53)55(64-52)79-34-44-33-67(21-23-78-44)20-8-6-7-9-22-75-24-25-76-26-27-77-35-49(70)62-51(57(3,4)5)56(72)68-32-43(69)29-47(68)54(71)59-30-39-11-13-40(14-12-39)50-38(2)60-36-80-50/h10-19,28,31,36,43-44,47,51,66,69H,6-9,20-27,29-30,32-35H2,1-5H3,(H,59,71)(H,62,70)(H,61,63,64,65)/t43-,44-,47+,51-/m1/s1
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| Chemical Name |
(2S,4R)-1-[(2S)-2-[[2-[2-[2-[6-[(2R)-2-[[6-[4-[(2-fluoro-5-methylphenyl)sulfonylamino]phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxymethyl]morpholin-4-yl]hexoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~86.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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