MS98
Based on 1 publication(s) in Google Scholar
MS98 is a AKT PROTAC degrader with a DC50 of 78 nM in BT474 cells. MS98 binds to purified AKT1, AKT2 and AKT3 isoforms with Kd values of 4 nM, 140 nM and 8 nM, respectively. MS98 recruits the VHL E3 ligase to induce polyubiquitination and proteasomal degradation of AKT. MS98 inhibits downstream signal transduction of the PI3K/AKT/m-TOR pathway. MS98 suppresses cancer cell proliferation. MS98 can be used for the research of prostate cancer and breast cancer.
(Pink: Akt ligand (HY-15186); Blue: VHL ligand (HY-112078); Black: linker).
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- CAS No.: 2376137-31-2
- Formule: C58H81ClN10O7S
- Masse moléculaire:1097.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) MS98
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Activité biologique
Description
IC50 & Target
[1]|
Akt1 4 nM (Kd) |
Akt2 140 nM (Kd) |
Akt3 8.1 nM (Kd) |
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | DC50 |
78 nM
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AKT degradation in human BT474 breast cancer cells assessed by western blot analysis of total AKT protein levels after 24 h incubation.
AKT degradation in human BT474 breast cancer cells assessed by western blot analysis of total AKT protein levels after 24 h incubation.
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34855399 |
| BT-474 | GI50 |
1.5 μM
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Antiproliferative activity against human BT474 breast cancer cells measured by cell proliferation inhibition assay.
Antiproliferative activity against human BT474 breast cancer cells measured by cell proliferation inhibition assay.
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34855399 |
In Vitro
MS98 (Compound 13) (100 nM-10 μM; 4-24 h) induces AKT degradation in BT474 breast cancer cells in a concentration- and time-dependent manner via the ubiquitin-proteasome system, with a DC50 of 78 nM, and this process requires the involvement of both AKT and the VHL E3 ligase[1].
MS98 induces AKT degradation in a concentration-dependent manner in PC3 prostate cancer cells and MDA-MB-468 breast cancer cells[1].
MS98 (1 μM; 24 h) selectively reduces the protein levels of AKT1 and AKT2 in BT474 breast cancer cells[1].
MS98 inhibits the proliferation of BT474 breast cancer cells, with a GI50 of 1.5 μM[1].
MS98 binds to the purified AKT1, AKT2, and AKT3 isoforms with high affinity, with Kd values of 4 nM, 140 nM, and 8 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT474 breast cancer cells
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Concentration:100 nM, 1 μM, 10 μM (24 h incubation); 1 μM (4 h, 8 h, 24 h incubation)
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Incubation Time:24 h (100 nM, 1 μM, 10 μM); 4 h, 8 h, 24 h (1 μM)
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Result:Concentration-dependently depleted cellular T-AKT with a DC50 of 78 nM.
Induced substantial T-AKT degradation at 100 nM, near-complete depletion at 1 μM, and no "hook effect" at concentrations up to 10 μM.
Induced rapid T-AKT degradation with obvious degradation at 4 h, near-complete degradation at 8 h, and sustained degradation for at least 24 h when treated at 1 μM.
Parmacokinetics
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 50 mg/kg | i.p. | 3.5 μM |
Chemical Information
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CAS No. 2376137-31-2
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Masse moléculaire 1097.84
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS98 Related Classifications
HY-145281 Related Classifications
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