MS5128
MS5128 is an OTUB1-based deubiquitinase-targeting chimera (DUBTAC) targeting CFTR. MS5128 recruits OTUB1 to CFTR to induce deubiquitination and stabilization of CFTR. MS5128 can be used for the research of cystic fibrosis. (Blue: CFTR Ligand (HY-183724); Pink: OTUB1 Ligand (HY-13262); Black: Linker)
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- No. CAS: 3060520-82-0
- Fòrmula: C49H55F2N7O7S
- Peso molecular:924.07
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
OTUB1 |
In Vitro
MS5128 (Compound 43) (0.5-10 μM; 3-24 h) increases ΔF508-CFTR protein levels in a concentration- and time-dependent manner in CFBE41o-4.7 ΔF508-CFTR cells, with maximal stabilization observed at 10 μM for 18 h, and this effect depends on engagement of both CFTR and OTUB1[1].
MS5128 (10 μM; 24 h) does not change CFTR mRNA levels in CFBE41o-4.7 ΔF508-CFTR cells after 24 h of treatment at 10 μM, indicating its CFTR-stabilizing effect is post-transcriptional[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CFBE41o-4.7 ΔF508-CFTR human cystic fibrosis bronchial epithelial cells
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Concentration:0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:3 h, 6 h, 12 h, 18 h, 24 h
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Result:Significantly increased the CFTR protein level compared to vehicle control after 24 h of treatment with 10 μM MS5128.
Increased the CFTR protein level in a time-dependent manner, with detectable elevation at 6 h and maximal stabilization at 18 h of treatment with 10 μM MS5128.
Abolished its CFTR-stabilizing effect when cotreated with either 25 μM Lumacaftor (HY-13262) or 25 μM compound 34 at 10 μM for 24 h.
Drastically reduced MS5128-induced CFTR stabilization when OTUB1 was depleted via lentiviral sgRNA transduction with 10 μM MS5128 for 24 h.
Chemical Information
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No. CAS 3060520-82-0
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Peso molecular 924.07
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Fòrmula C49H55F2N7O7S
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SMILES
O=C(C1=CC=CC(C2=NC(NC(C3(CC3)C4=CC=C5OC(F)(OC5=C4)F)=O)=CC=C2C)=C1)NCCCCCCNC(CCC6=CC=C(S6)C(N7CC8CC(C7)N8C(/C=C/CN(C)C)=O)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS5128 Related Classifications
HY-183725 Related Classifications
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