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Cat. No.: HY-143883

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MS143

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MS143 is a potent PROTAC AKT degrader (DC₅₀=46 nM and GI₅₀=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth.
(Pink: Akt ligand (HY-15431); Blue: VHL ligand (HY-125845); Black: linker).

For research use only. We do not sell to patients.

CAS No.: 2376137-41-4
Formula: C₅₉H₈₁ClN₁₂O₆S
Molecular Weight:1121.87

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS143 Chemical Structure

CAS No.: 2376137-41-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

MS143 is a potent PROTAC AKT degrader (DC₅₀=46 nM and GI₅₀=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth^[1]. (Pink: Akt ligand (HY-15431); Blue: VHL ligand (HY-125845); Black: linker).

IC₅₀ & Target

AKT

All PROTACs Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-468	GI₅₀	1 μM Compound: 20; , MS143	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth by measured after 5 days by IncuCyte zoom live cell analysis Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth by measured after 5 days by IncuCyte zoom live cell analysis	[PMID: 35119851]
PC-3	GI₅₀	0.8 μM Compound: 20; , MS143	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 5 days by IncuCyte zoom live cell analysis Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 5 days by IncuCyte zoom live cell analysis	[PMID: 35119851]

In Vitro

MS143 (1 nM-10 μM; 24 hours) induces T-AKT degradation with a concentration-dependent manner in PC3 cells^[1].
MS143 (0.1-10 μM;14 days, replenish every 2 days) effectively inhibits colony formation in BT474 cells^[1].
MS143 (1 μM; 24 hours) promotes AKT degradation in an E3 ligase- and UPS-dependent manner^[1].
MS143 (1 nM-10 μM) can inhibit the cell growth of PC3 cells (GI₅₀=0.8 nM) and MDA-MB-468 cells (GI₅₀=1.0 nM)^[1].

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

Cell Proliferation Assay

Cell Line:

PC3 cells and MDA-MB-468 cells^[1]
Concentration:

1 nM, 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:

5 days
Result:

Inhibited the cell growth of PC3 cells (GI₅₀=0.8 nM) and MDA-MB-468 cells (GI₅₀=1.0 nM).

Western Blot Analysis

Cell Line:

PC3 cells^[1]
Concentration:

1 μM
Incubation Time:

24 hours
Result:

Promoted AKT degradation in an E3 ligase- and UPS-dependent manner.

In Vivo

MS143 (75 mg/kg; i.p., 22 days) drastically inhibits the tumor growth by 92%, also substantially degrades T-AKT and P-AKT, and effectively inhibits the downstream signaling (PRAS40 phosphorylation) in xenograft mice^[1].
Pharmacokinetic Parameters of MS143 in male Swiss Albino mice^[1].

	IP (75 mg/kg)
C_max (μM)	7
T_max (h)	2
AUC_0-12 (h·ng/mL)	63600

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

Animal Model:

Male immunocompromised NU/J mice (6 weeks old)^[1]
Dosage:

75 mg/kg
Administration:

i.p., 22 days
Result:

Drastically inhibited the tumor growth by 92%, also substantially degraded T-AKT and P-AKT, and effectively inhibited the downstream signaling (PRAS40 phosphorylation).

Chemical Information

CAS No. 2376137-41-4
Appearance Solid
Molecular Weight 1121.87
Formula C₅₉H₈₁ClN₁₂O₆S
Color White to off-white
SMILES

O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(CCCCCCCCCCC(N(CC4)CCN4CC[C@@H](C5=CC=C(C=C5)Cl)NC(C6(CCN(CC6)C7=C8C(NC=C8)=NC=N7)N)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. Yu X, et al. Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies. J Med Chem. 2022;65(4):3644-3666. [Content Brief]

Calculators

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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

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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MS143

All PROTACs Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

MS143 Related Classifications

HY-143883 Related Classifications