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MS98

Catalog No. T39930 CAS 2376137-31-2

MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM.

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MS98, CAS 2376137-31-2

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25 mg	Inquiry	$ 1,520.00

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Biological Description

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Description	MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM.
Targets&IC50	Akt3:8.1 nM, Akt2:140 nM, Akt1:4 nM
In vitro	The von Hippel-Lindau (VHL)-recruiting degrader MS98 is a potent AKT degrader that effectively induces AKT protein degradation and inhibits its downstream signaling pathways, leading to the suppression of cancer cell proliferation. By employing the ubiquitin-proteasome system (UPS), MS98 achieves concentration- and time-dependent degradation of AKT. Specifically, MS98, within the concentration range of 10 nM to 10 μM, significantly inhibits proliferation across various cancer cell lines. Additionally, it concentration-dependently depletes cellular total AKT (T-AKT) with a DC50 value of 78±64 nM. Cell viability assays revealed that MS98, at concentrations ranging from 10 nM to 10 μM over five days, inhibited cell growth in BT474, PC3, and MDA-MB-468 cells with GI50 values of 1.3±0.3 μM, 9.2±1.3 μM, and 3.8±1.2 μM, respectively. Furthermore, Western Blot analysis on BT474 cells, with MS98 concentrations from 1 nM to 10 μM over 24 hours, demonstrated a potent induction of AKT degradation, highlighting MS98's efficacy in cancer cell growth inhibition through AKT protein degradation mechanisms.
In vivo	MS98, administered through a single intraperitoneal (IP) injection at a dosage of 50 mg/kg, exhibits bioavailability in male Swiss albino mice. Pharmacokinetic analysis reveals that the maximum plasma concentration (C max) of approximately 3.5 μM is achieved 2 hours post-injection, with plasma levels remaining above 3 μM for a duration of over 8 hours.

Molecular Weight	1097.86
Formula	C58H81ClN10O7S
CAS No.	2376137-31-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Yu X, et al. Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders. J Med Chem. 2021;64(24):18054-18081.

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Keywords

MS98 2376137-31-2 MS-98 MS 98 inhibitor inhibit

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