2. PROTAC Cell Cycle/DNA Damage Membrane Transporter/Ion Channel
  3. DUBTACs Deubiquitinase CFTR
  4. 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)

For research use only. We do not sell to patients.

MS5128

MS5128 Chemical Structure

CAS No. : 3060520-82-0

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MS5128 Related Antibodies

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Description

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[1]. (Blue: CFTR Ligand (HY-183724); Pink: OTUB1 Ligand (HY-13262); Black: Linker)

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.

MS5128 Related Antibodies

Western Blot Analysis[1]

Cell Line: CFBE41o-4.7 ΔF508-CFTR human cystic fibrosis bronchial epithelial cells
Concentration: 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time: 3 h, 6 h, 12 h, 18 h, 24 h
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.
Molecular Weight

924.07

Formula

C49H55F2N7O7S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS5128 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS51283060520-82-0MS 5128MS-5128DUBTACsDeubiquitinaseCFTRDeubiquitinase-targeting chimerasDUBsCystic fibrosis transmembrane conductance regulatorcysteine 23deubiquitinase-targeting chimeraΔF508-CFTRCFBE41o-4.7 ΔF508-CFTR cellsOTUB1cystic fibrosisInhibitorinhibitorinhibit

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