SK-3-91
Based on 1 Customer Validation
SK-3-91 is a PROTAC-type multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). SK-3-91 induces protein (YTHDF2, e.g.) degradation through the ubiquitin biotinylation (E-STUB) pathway. SK-3-91 degrades YTHDF2. SK-3-91 inhibits cell proliferation and induces morphological changes.
(Pink: YTHDF2 ligand (HY-169396); Blue: Cereblon ligand (HY-131717); Black: linker (HY-140819)).
For research use only. We do not sell to patients.
- Purity: 98.33%
- CAS No.: 2769753-23-1
- Formula: C42H47ClN10O8S
- Molecular Weight:887.40
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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YTHDF2 |
SK-3-91 (0.12-10 μM, 24 h) degrades YTHDF2 at the sub-micromolar concentrations in K562 cells[2].
SK-3-91 (1-50 μM) shows significantly less cytotoxicity against the U2OS cells at the higher concentrations of either 3 μM or 10 μM[2].
SK-3-91 (400 nM, 72 h) inhibits cell proliferation in K562 cells[2].
SK-3-91(1-10 μM, 20 h) induces morphological changes in U2OS cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:400 nM
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Incubation Time:72 h
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Result:Showed inhibition of 88.2%.
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Cell Line:K562 cells
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Concentration:0.12, 0.37, 1.1, 3.3, 10 μM
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Incubation Time:24 h
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Result:Degraded YTHDF2 at the sub-micromolar concentrations.
Chemical Information
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CAS No. 2769753-23-1
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Appearance Solid
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Molecular Weight 887.40
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Formula C42H47ClN10O8S
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Color Light yellow to yellow
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SMILES
O=C(N1C2C(NC(CC2)=O)=O)C3=C(NCC(NCCOCCN4CCN(C5=CC=C(NC6=NC(NC7=C(S(C(C)C)(=O)=O)C=CC=C7)=C(Cl)C=N6)C=C5)CC4)=O)C=CC=C3C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 200 mg/mL (225.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (5.63 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (5.63 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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 (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Donovan KA, et al. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020 Dec 10;183(6):1714-1731.e10. [Content Brief]
[2]. Goebel GL, et al. Profiling Cellular Morphological Changes Induced by Dual-Targeting PROTACs of Aurora Kinase and RNA-Binding Protein YTHDF2. Chembiochem. 2024 Oct 1;25(19):e202400183. [Content Brief]
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 (protect from light). 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 | 1.1269 mL | 5.6344 mL | 11.2689 mL | 28.1722 mL |
| 5 mM | 0.2254 mL | 1.1269 mL | 2.2538 mL | 5.6344 mL | |
| 10 mM | 0.1127 mL | 0.5634 mL | 1.1269 mL | 2.8172 mL | |
| 15 mM | 0.0751 mL | 0.3756 mL | 0.7513 mL | 1.8781 mL | |
| 20 mM | 0.0563 mL | 0.2817 mL | 0.5634 mL | 1.4086 mL | |
| 25 mM | 0.0451 mL | 0.2254 mL | 0.4508 mL | 1.1269 mL | |
| 30 mM | 0.0376 mL | 0.1878 mL | 0.3756 mL | 0.9391 mL | |
| 40 mM | 0.0282 mL | 0.1409 mL | 0.2817 mL | 0.7043 mL | |
| 50 mM | 0.0225 mL | 0.1127 mL | 0.2254 mL | 0.5634 mL | |
| 60 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.4695 mL | |
| 80 mM | 0.0141 mL | 0.0704 mL | 0.1409 mL | 0.3522 mL | |
| 100 mM | 0.0113 mL | 0.0563 mL | 0.1127 mL | 0.2817 mL |
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