LY3200882 |
| カタログ番号GC19234 |
LY3200882 は、38.2 nM の IC50 を持つ、強力で高度に選択的な ATP 競合性および経口活性 TGF-β 受容体 1 (ALK5) 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1898283-02-7
Sample solution is provided at 25 µL, 10mM.
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LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
LY3200882 is a novel, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells. LY3200882 has shown anti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation[1].
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)[1].
References:
[1]. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955.
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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