2376137-31-2
2376137-31-2 structure
- Name: MS98
- Chemical Name: MS98
- CAS Number: 2376137-31-2
- Molecular Formula: C58H81ClN10O7S
- Molecular Weight: 1097.84
- Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
- Create Date: 2022-05-21 19:40:34
- Modify Date: 2024-01-04 11:30:14
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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[1].
| Name | MS98 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
Akt1:4 nM () Akt2:140 nM () Akt3:8.1 nM () VHL |
| In Vitro | 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]. Cell Viability Assay[1] Cell Line: BT474, PC3, and MDA-MB-468 cells Concentration: 10 nM, 100 nM, 1 μM, 10 μM Incubation Time: 5 days 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. Western Blot Analysis[1] Cell Line: BT474 cells Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM , 3 μM, and 10 μM Incubation Time: 24 hours Result: Potently induced AKT degradation. |
| In Vivo | MS98 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection. The maximum plasma concentration (Cmax) reaches approximately 3.5 μM at 2 h, and the plasma concentrations remains above 3 μM over 8 h[1]. Animal Model: Male Swiss albino mice[1] Dosage: Single 50 mg/kg(Pharmacokinetic Analysis) Administration: IP injection over 8 h Result: Bioavailable in mouse PK studies. The Cmax is 3.5 μM at 2 h. |
| References |
| Molecular Formula | C58H81ClN10O7S |
|---|---|
| Molecular Weight | 1097.84 |