| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC-based degrader of SKG3 (Serum/Glucocorticoid Regulated Kinase Family Member 3), inducing 50% degradation of endogenous SGK3 in 2 hours, with maximal 80% degradation occurred within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
| 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].
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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. |
| References |
| 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
|
| PubChem CID |
139035049
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| Appearance |
White to off-white solid powder
|
| LogP |
6
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
29
|
| Heavy Atom Count |
81
|
| Complexity |
2050
|
| Defined Atom Stereocenter Count |
4
|
| 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
|
| 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
|
| 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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