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製品番号: HY-145281

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MS98

1 Cited Publications

カスタマーレビュー

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 番号: 2376137-31-2
分子式: C₅₈H₈₁ClN₁₀O₇S
分子量:1097.84

保管条件:

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

Data Sheet (271 KB)

MS98 構造式

CAS 番号: 2376137-31-2

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数量

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (1)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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

PROTACs アイソフォーム固有の製品をすべて表示 :

Akt アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2376137-31-2
分子量 1097.84
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (271 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

MS98

1 Cited Publications

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (1)
純度とドキュメンテーション
参考文献

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MS98

MedChemExpress（MCE）の使用を引用している文献 MS98

PROTACs アイソフォーム固有の製品をすべて表示

Akt アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

MS98 関連分類

HY-145281 関連分類