2. PROTAC PI3K/Akt/mTOR
  3. PROTACs Akt
  4. MS15

MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.

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MS15

MS15 構造式

CAS 番号 : 3035638-40-2

容量 価格（税別） 在庫状況
1 mg $380 見積もりとリードタイムを求めるのご確認
5 mg $930 見積もりとリードタイムを求めるのご確認
10 mg $1480 見積もりとリードタイムを求めるのご確認

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Other 在庫あり Forms of MS15:

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MS15 関連抗体

Top Publications Citing Use of Products

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Akt アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Akt Akt1 Akt2 Akt3

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製品説明

MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively[1].

IC50 & Target

Akt2

90 ± 2.8 nM (IC50)

Akt3

544 ± 2.9 nM (IC50)

Akt1

798 ± 190 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
SW-620 GI50
3.1 μM
Compound: 62; MS15
Antiproliferative activity against human SW620 cells harboring KRAS mutant assessed as inhibition of cell growth incubated for 5 days by IncuCyte live-cell imaging analysis
Antiproliferative activity against human SW620 cells harboring KRAS mutant assessed as inhibition of cell growth incubated for 5 days by IncuCyte live-cell imaging analysis
[PMID: 36197750]
体外実験

MS15 (0-10 μM, 24 h) potently induces AKT degradation in SW620 cells and MS21-resistant KRAS/BRAF mutant cells[1].
MS15 (0-10 μM, 5 days) inhibits the proliferation of KRAS mutant SW620 cells[1].
MS15 (1 μM, 1-24 h) mediates AKT degradation in a time- and UPS-dependent manner[1].

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

MS15 関連抗体

Western Blot Analysis[1]

Cell Line: SW620 cells, Colo205, HT-29, SKMEL 239, and PANC-1 cells
Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
Incubation Time: 24 h
Result: Effectively induced T-AKT degradation in a concentration-dependent manner, with a DC50 value of 23 ± 16 nM in SW620 cells. Nearly complete AKT degradation was achieved at a concentration of 100 nM in SW620 cells and PANC-1 cells. Induced AKT degradation at 1 μM in BRAF mutant cell lines, such as Colo205, HT-29, and SKMEL 239 cells.

Cell Proliferation Assay[1]

Cell Line: SW620 cells
Concentration: 0 nM, 30 nM, 100 nM, 1 μM, 3 μM, 10 μM
Incubation Time: 5 days
Result: Displayed slightly better antiproliferative activity than Miransertib (HY-19719), with a GI50 of 3.1 ± 0.3 μM.
体内実験

MS15 (75 mg/kg, IP, once) is bioavailable in mice through intraperitoneal administration[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: 75 mg/kg
Administration: IP, once (Pharmacokinetic Analysis)
Result: The maximum plasma concentration (Cmax = 1 μM) was achieved at 0.5 h post-treatment, and plasma concentrations were maintained above 100 nM for at least 12 h.Could achieve enough plasma exposure for effective AKT degradation.
分子量

1114.45

分子式

C64H79N11O5S
CAS 番号
SMILES

NC1(CCC1)C(C=C2)=CC=C2N3C4=NC(C5=CC(CCC(NCCCCCCCCCCC(N[C@H](C(N6C[C@@H](C[C@H]6C(N[C@@H](C)C7=CC=C(C=C7)C8=C(N=CS8)C)=O)O)=O)C(C)(C)C)=O)=O)=CC=C5)=CC=C4N=C3C9=CC=CN=C9N
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.
純度とドキュメンテーション
参考文献
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MS15 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:

MS153035638-40-2MS 15MS-15PROTACsAktPKBProtein kinase BKRAS/BRAFcancerSW620 cellsColo205HT-29SKMEL 239PANC-1 cellsInhibitorinhibitorinhibit

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