PROTAC MPS1 degrader 1
Based on 1 Customer Validation
PROTAC MPS1 degrader 1 is a selective monopolar spindle 1 (Mps1/TTK) PROTAC degrader, with DC50 values of 17.7, 108.67 and 570.25 nM against TTK, AURKA and AURKB, respectively. PROTAC MPS1 degrader 1 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC MPS1 degrader 1 can be used in research related to acute myeloid leukemia.
(Pink: Mps1 ligand (HY-168542); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W141926)).
For research use only. We do not sell to patients.
- Purity : 99.90%
- Formula: C41H46N12O7
- Molecular Weight:818.88
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TTK 17.7 nM (DC50) |
Aurora A 108.7 nM (DC50) |
Aurora B 570.3 nM (DC50) |
Cereblon |
In Vitro
PROTAC MPS1 degrader 1 (Compound 19) (6 h) potently degrades TTK in MV4-11HiBiT-TTK cells, with a DC50 of 17.7 nM and a Dmax of 66.5% after 6 hours of treatment[1].
PROTAC MPS1 degrader 1 (6 h) degrades HiBiT-tagged AURKA in MV4-11AURKA-HiBiT cells, with a DC50 of 109 nM and a Dmax of 78.8% after 6 hours of treatment[1].
After 6 h of treatment, PROTAC MPS1 degrader 1 (6 h) degrades HiBiT-tagged AURKB in MV4-11AURKB-HiBiT cells, with a DC50 of 570 nM and a Dmax of 43.6%[1].
PROTAC MPS1 degrader 1 (0.04-10 μM; 6 h) induces significant, dose-dependent degradation of endogenous TTK and AURKA in untreated MV4-11 cells after 6 hours of treatment[1].
PROTAC MPS1 degrader 1 (1-10 μM; 6 h) induces the degradation of TTK, AURKA and AURKB in untreated MV4-11 cells via a proteasome-dependent CRBN recruitment mechanism[1].
PROTAC MPS1 degrader 1 (0.1-10 μM; 6 h) upregulates TTK mRNA levels and downregulates AURKA and AURKB mRNA levels in untreated MV4-11 cells after 6 hours of treatment, indicating that TTK protein degradation is not driven by decreased transcription[1].
PROTAC MPS1 degrader 1 (72 h) reduces the viability of untreated MV4-11 cells, with an EC50 of 1.4 μM following 72 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:naive MV4-11 acute myeloid leukemia cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:6 h
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Result:Increased TTK mRNA levels at all tested concentrations.
Decreased AURKA mRNA levels in a concentration-dependent manner, to 66-85% of vehicle levels at 10 μM.
Decreased AURKB mRNA levels in a concentration-dependent manner, to 72-80% of vehicle levels at 10 μM.
Chemical Information
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Appearance Solid
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Molecular Weight 818.88
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Formula C41H46N12O7
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Color Off-white to gray
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SMILES
O=C(NCC(N1CCN(C2=CC=C(NC3=NC(NC4CCCCC4)=C5N=CNC5=N3)C=C2)CC1)=O)CCCC(NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (122.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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
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. 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 |
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| DMSO | 1 mM | 1.2212 mL | 6.1059 mL | 12.2118 mL | 30.5295 mL |
| 5 mM | 0.2442 mL | 1.2212 mL | 2.4424 mL | 6.1059 mL | |
| 10 mM | 0.1221 mL | 0.6106 mL | 1.2212 mL | 3.0530 mL | |
| 15 mM | 0.0814 mL | 0.4071 mL | 0.8141 mL | 2.0353 mL | |
| 20 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5265 mL | |
| 25 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | 1.2212 mL | |
| 30 mM | 0.0407 mL | 0.2035 mL | 0.4071 mL | 1.0177 mL | |
| 40 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7632 mL | |
| 50 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6106 mL | |
| 60 mM | 0.0204 mL | 0.1018 mL | 0.2035 mL | 0.5088 mL | |
| 80 mM | 0.0153 mL | 0.0763 mL | 0.1526 mL | 0.3816 mL | |
| 100 mM | 0.0122 mL | 0.0611 mL | 0.1221 mL | 0.3053 mL |
PROTAC MPS1 degrader 1 Related Classifications
HY-168540 Related Classifications
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