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Art. -Nr.: HY-145281

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MS98

1 Cited Publications

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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 K_ds 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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CAS. Nr.: 2376137-31-2
Formel: C₅₈H₈₁ClN₁₀O₇S
Molecular Weight:1097.84

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

MS98 Chemical Structure

CAS. Nr.: 2376137-31-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 K_ds of 4 nM, 140 nM, and 8.1 nM, respectively^[1]. (Pink: Akt ligand (HY-15186); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target

Akt1

4 nM ()

Akt2

140 nM ()

Akt3

8.1 nM ()

VHL

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-474	GI₅₀	1.3 μM Compound: 13; MS98	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	[PMID: 34855399]
MDA-MB-468	GI₅₀	3.8 μM Compound: 13; MS98	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	[PMID: 34855399]
PC-3	GI₅₀	9.2 μM Compound: 13; MS98	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	[PMID: 34855399]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (C_max) reaches approximately 3.5 μM at 2 h, and the plasma concentrations remains above 3 μM over 8 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max is 3.5 μM at 2 h.

Chemical Information

CAS. Nr. 2376137-31-2
Molecular Weight 1097.84
Formel C₅₈H₈₁ClN₁₀O₇S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Journal Impact Factor

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise

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MS98

Publications Citing Use of MedChemExpress (MCE) MS98

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen