LY2109761 --- TGFβ Inhibitor.
| Overview | |
| Catalog # | bs-60035c-10mg-solid |
| Product Name | LY2109761 --- TGFβ Inhibitor. |
| Specifications | |
| Storage Buffer | Powder |
| Storage Condition | Store in dry, dark place at -20C for 1 year. |
| Target | |
| Product Information | Molecular Weight: 441.52 Formula: C26 H27 N5 O2 CAS Number: 700874-71-1 InChi Key: IHLVSLOZUHKNMQ-UHFFFAOYSA-N InChi: InChI=1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2 Smiles: C(COC1C=C2N=CC=C(C3C(=NN4CCCC4=3)C3C=CC=CN=3)C2=CC=1)N1CCOCC1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
| Description | LY2109761 is a highly potent and selective TGFβ receptor type I and type II (TβRI/II) inhibitor with Ki of 38 nM and 300 nM respectively. Blocking TβRI/II kinase activity with LY2109761 completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, and completely suppresses TGF-β–induced Smad2 phosphorylation. LY2109761 treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. It can also reduce the self-renewal and proliferation of GBM-derived cancer stem–like cells, which can be significantly enhanced when combined with radiation. Administration of LY2109761 alone or in combination with gemcitabine or with radiation demonstrated very good efficacy in multiple xenograft mice models. |
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