2. PI3K/Akt/mTOR
  3. Akt
  4. MS143

MS143 is a potent 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.

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MS143 Chemical Structure

MS143 Chemical Structure

CAS No. : 2376137-41-4

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MS143 Related Antibodies

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Description

MS143 is a potent 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].

IC50 & Target

AKT
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.

MS143 Related Antibodies

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)
Cmax (μM) 7
Tmax (h) 2
AUC0-12 (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).
Molecular Weight

1121.87

Formula

C59H81ClN12O6S
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS143 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS1432376137-41-4MS 143MS-143AktPKBProtein kinase BAKTDegradationUbiquitin-proteasome systemCancerPC3 cellsXenograft modelInhibitorinhibitorinhibit

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