Cat. No. Name Size Price Add Cart
KI0505LY21097615 mg$432
LY210976110 mg$592
LY210976150 mg$1712
LY2109761200 mg$3952

Chemical Characteristic

Product NameLY2109761
CAS No.700874-71-1
Molecular Weight 441.52
FormulaC26H27N5O2
Chemical Name4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]quinoline
Smilesn1ccc(c2ccc(cc12)OCCN1CCOCC1)c1c2n(nc1c1ccccn1)CCC2
Chemical Structure

Biological activities

LY2109761 is a selective chemical competitive inhibitor of the transforming growth factor β Type II receptor (TβR) kinases. The IC50 of LY2109761 is 0.3 μM against TβRII. LY2109761 targets both the TβRII and TβRI kinases but does not affect BMP-induced cellular responses. In HaCaT cells, treatment with LY2109761 generates rapid dephosphorylation of all TGFβ-activated R-Smads. In sharp contrast to the lack of effect of SD-093 on pSmad1 and pSmad5 levels in A253 cells, treatment with LY2109761 results in rapid dephosphorylation of these BMP-Smads. More importantly, LY2109761 treatment results in redistribution of F-actin toward the cell periphery and of E-cadherin to the cell membrane. Treatment of A253 cells with LY2109761 alone (in the absence of exogenous TGFβ) induces a more cohesive epithelioid morphology with distinct cell boundaries. LY2109761 at the dose of 1 μM inhibits invasion by ∼50% independently of the presence of TGFβ. LY2109761 also inhibits 3TP-lux activity.[1] LY2109761 markedly reduces inflammation and pulmonary fibrosis resulting in prolonged survival. LY2109761 reduces p-SMAD2 and p-SMAD1 expression. LY2109761 suppresses expression of genes involved in canonical and noncanonical TGF-β signaling and downstream signaling of bone morphogenetic proteins (BMP).[2] LY2109761 reduces clonogenic survival of U87 and T98 cells and further enhances the radiation-induced anticlonogenicity. LY2109761 has antimigratory and antiangiogenic effects in Matrigel migration and tube formation assays. In vivo, in human xenograft tumors growing subcutaneously on BALB/c nu/nu mice, LY2109761 suppresses tumor growth. LY2109761 also reduces tumor blood perfusion as quantified by noninvasive dynamic contrast-enhanced magnetic resonance imaging.[3]

Protocols

LY2109761 is dissolved in DMSO.[1]

References

[1] Bharathy S, et al. Cancer-associated transforming growth factor beta type II receptor gene mutant causes activation of bone morphogenic protein-Smads and invasive phenotype. Cancer Res. 2008, 68(6): 1656-1666.
[2] Flechsig P, et al. LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signals. Clin Cancer Res. 2012, 18(13): 3616-3627.
[3] Zhang M, et al. Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-β receptor I kinase inhibitor LY2109761. Neoplasia. 2011, 13(6): 537-549.

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