1. Epigenetics TGF-beta/Smad
  2. PKC
  3. MT477

MT477 is a potent protein kinase C (PKC) inhibitor. MT477 induces apoptosis and necrosis. MT477 decreases the protein expression of Ras-GTP, p-Erk1/2, p-Elk1. MT477 shows antitumor activity.

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MT477

MT477 構造式

CAS 番号 : 328069-91-6

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製品説明

MT477 is a potent protein kinase C (PKC) inhibitor. MT477 induces apoptosis and necrosis. MT477 decreases the protein expression of Ras-GTP, p-Erk1/2, p-Elk1. MT477 shows antitumor activity[1].

体外実験

MT477 (0.05 mM; 1, 24 h) induces apoptosis and necrosis in a time-dependent manner[1].
MT477 (0.05 mM; 0.5, 1, 2, 4 h) decreases the protein expression of Ras-GTP, p-Erk1/2, p-Elk1 in a time-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7, U87, H226, LNCaP, A549, A431 cells
Concentration: 0.001-1 mM
Incubation Time: 1 h
Result: Showed antiproliferative activity with IC50s of 0.018, 0.051, 0.013, 0.033, 0.020, 0.049 mM for MCF-7, U87, H226, LNCaP, A549, A431 cells, respectively.

Western Blot Analysis[1]

Cell Line: H266 cells
Concentration: 0.05 mM
Incubation Time: 0.5, 1, 2, 4 h
Result: Decreased the protein expression of Ras-GTP, p-Erk1/2, p-Elk1 in a time-dependent manner.

Apoptosis Analysis[1]

Cell Line: H266 cells
Concentration: 0.05 mM
Incubation Time: 1, 24 h
Result: Induced apoptosia with the percentage of cells underwent apoptosis after 1 h of treatment of 18.6 and after 24 h of treatment of 98%.
体内実験

MT477 (33, 100, 1000 µg/kg; i.p.; once a day on days 1, 4, 8, 16, 18, 20) shows antitumor activity[1].

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

Animal Model: 6-week-old male nude mice (A431 cells) [1]
Dosage: 33, 100, 1000 µg/kg
Administration: I.p.; once a day on days 1, 4, 8, 16, 18, 20
Result: Significant decreased in tumor volume of 24.5% by the third week at 1 mg/kg.
Animal Model: 6-week-old male nude mice (H226 cells) [1]
Dosage: 1 mg/kg
Administration: I.p.; once a day on days 1, 4, 8, 20, 24, 28
Result: Inhibited tumor growth by 43.6% and observed no weight loss.
分子量

718.77

分子式

C31H30N2O12S3

CAS 番号
SMILES

O=C(OC)C1=C(SC2=C(C3=C(C(OC)=CC=C3)N(C2(C)C)C(CN4C(CCC4=O)=O)=O)C15SC(C(OC)=O)=C(S5)C(OC)=O)C(OC)=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.

純度とドキュメンテーション
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  • 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.

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製品名:
MT477
製品番号:
HY-122241
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