MS98
Based on 1 publication(s) in Google Scholar
MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds of 4 nM, 140 nM, and 8.1 nM, respectively.
(Pink: Akt ligand (HY-15186); Blue: VHL ligand (HY-112078); Black: linker).
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- No. CAS: 2376137-31-2
- Fòrmula: C58H81ClN10O7S
- Peso molecular:1097.84
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) MS98
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Actividad biológica
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Akt1 4 nM () |
Akt2 140 nM () |
Akt3 8.1 nM () |
VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | GI50 |
1.3 μM
Compound: 13; MS98
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Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human BT-474 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
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[PMID: 34855399] |
| MDA-MB-468 | GI50 |
3.8 μM
Compound: 13; MS98
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Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
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[PMID: 34855399] |
| PC-3 | GI50 |
9.2 μM
Compound: 13; MS98
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Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 5 days by IncuCyte live-cell imaging analysis
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[PMID: 34855399] |
The von Hippel-Lindau (VHL)-recruiting degrader MS98 is an effective AKT degrader. MS98 selectively induces robust AKT protein degradation, inhibits downstream signaling, and suppresses cancer cell proliferation. MS98 concentration- and time-dependently induces AKT degradation through the ubiquitin-proteasome system (UPS)[1].
MS98 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines[1].
MS98 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC50 value of 78±64 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT474, PC3, and MDA-MB-468 cells
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Concentration:10 nM, 100 nM, 1 μM, 10 μM
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Incubation Time:5 days
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Result:Inhibited the cell growth with GI50s of 1.3±0.3 μM, 9.2±1.3 μM, and 3.8±1.2 μM for BT474 cells, PC3 cells, and MDA-MB-468 cells, respectively.
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Cell Line:BT474 cells
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Concentration:1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM , 3 μM, and 10 μM
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Incubation Time:24 hours
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Result:Potently induced AKT degradation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss albino mice[1]
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Dosage:Single 50 mg/kg(Pharmacokinetic Analysis)
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Administration:IP injection over 8 h
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Result:Bioavailable in mouse PK studies. The Cmax is 3.5 μM at 2 h.
Chemical Information
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No. CAS 2376137-31-2
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Peso molecular 1097.84
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Fòrmula C58H81ClN10O7S
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SMILES
C[C@H]1C2=C(N3CCN(CC3)C([C@@H](C4=CC=C(C=C4)Cl)CNCCNC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O)=O)=O)N=CN=C2[C@@H](C1)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.
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Omega
Dynamic Detection of the E3-PROTAC-Target Protein Ternary Complex In Vitro and In Vivo via Bimolecular Fluorescence Complementation. [Abstract]2024 Dec 3;9(50):49739-49748. PMID: 39713624
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS98 Related Classifications
HY-145281 Related Classifications
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