LY2109761
Based on 71 publication(s) in Google Scholar
LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 700874-71-1
- Formula: C26H27N5O2
- Molecular Weight:441.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) LY2109761
More- J Hepatol. 2015 Oct;63(4):863-73. [Abstract]
- Cell Res. 2020 Jul;30(7):610-622. [Abstract]
- Hepatology. 2022 Oct;76(4):967-981. [Abstract]
- Nat Commun. 2025 Sep 10;16(1):8049. [Abstract]
- Nat Commun. 2017 Aug 18;8(1):286. [Abstract]
- Sci Transl Med. 2020 Mar 25;12(536):eaay8456. [Abstract]
- J Exp Clin Cancer Res. 2022 Aug 26;41(1):259. [Abstract]
- Int J Biol Sci. 2019 Sep 7;15(11):2393-2407. [Abstract]
- Cell Commun Signal. 2026 Feb 9;24(1):167. [Abstract]
- Int J Biol Macromol. 2026 Apr:356:151571. [Abstract]
- Acta Pharmacol Sin. 2022 Jan;43(1):133-145. [Abstract]
- Sci Total Environ. 2020 Aug 20;731:139234. [Abstract]
- J Transl Med. 2025 May 9;23(1):524. [Abstract]
- Biomed Pharmacother. 2023 Sep:165:115225. [Abstract]
- Biomed Pharmacother. 2020 Oct:130:110610. [Abstract]
- Cell Death Discov. 2025 Mar 15;11(1):104. [Abstract]
- Cell Death Discov. 2023 May 13;9(1):161. [Abstract]
- Cell Rep. 2026 Jun 18;45(7):117568. [Abstract]
- Cell Rep. 2026 Mar 27;45(4):117189. [Abstract]
- Cell Rep. 2020 Apr.
- J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]
- Phytother Res. 2024 Nov 12. [Abstract]
- JCI Insight. 2024 Jun 25:e175416. [Abstract]
- Ecotoxicol Environ Saf. 2023 May:256:114892. [Abstract]
- Ecotoxicol Environ Saf. 2021 Nov 30:228:113040. [Abstract]
- J Dent Res. 2019 Jul;98(8):896-903. [Abstract]
- Int J Mol Med. 2020 Jul;46(1):167-178. [Abstract]
- Int J Mol Med. 2015 Jun;35(6):1667-74. [Abstract]
- Cell Prolif. 2024 Jul 18:e13719. [Abstract]
- Biochem Pharmacol. 2024 Jun:224:116234. [Abstract]
- Biochem Pharmacol. 2023 Oct:216:115796. [Abstract]
- Life Sci. 2025 Oct 9:382:124008. [Abstract]
- Life Sci. 2023 Jun 15:323:121657. [Abstract]
- Int J Mol Sci. 2025 Jan 4;26(1):395. [Abstract]
- Int J Mol Sci. 2023 Jul 21;24(14):11766. [Abstract]
- Am J Physiol Cell Physiol. 2026 Feb 1;330(2):C467-C481. [Abstract]
- Int Immunopharmacol. 2022 Dec;113(Pt A):109396. [Abstract]
- Invest Ophthalmol Vis Sci. 2021 Jul 1;62(9):29. [Abstract]
- Int Immunopharmacol. 2020 Aug;85:106686. [Abstract]
- Mol Nutr Food Res. 2024 Feb;68(4):e2200726. [Abstract]
- J Cell Mol Med. 2024 Feb;28(3):e18059. [Abstract]
- J Cell Mol Med. 2021 Apr;25(7):3498-3510. [Abstract]
- FEBS J. 2020 Feb;287(4):783-799. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Abstract]
- J Inherit Metab Dis. 2025 Nov;48(6):e70111. [Abstract]
- J Virol. 2025 Jun 25:e0063825. [Abstract]
- Mol Cell Biochem. 2020 Jul;470(1-2):215-227. [Abstract]
- Mol Cell Biochem. 2019 Jun;456(1-2):95-104. [Abstract]
- Am J Pathol. 2023 Aug;193(8):1029-1045. [Abstract]
- Int J Med Sci. 2025 Mar 31;22(9):2031-2039. [Abstract]
- Pathol Res Pract. 2025 Mar 23:269:155899. [Abstract]
- Front Biosci (Landmark Ed). 2025 Nov 27;30(11):45591. [Abstract]
- Front Biosci (Landmark Ed). 2024 Sep 24;29(9):336. [Abstract]
- Cell Biol Int. 2017 Sep;41(9):960-968. [Abstract]
- Mol Immunol. 2018 Nov:103:173-181. [Abstract]
- Brain Sci. 2021 Jan 8;11(1):77. [Abstract]
- J Cell Biochem. 2019 Oct;120(10):17872-17886. [Abstract]
- Photochem Photobiol. 2024 Nov-Dec;100(6):1874-1893. [Abstract]
- Exp Ther Med. 2022 Jun 7;24(2):496. [Abstract]
- Exp Ther Med. 2021 Jan;21(1):6. [Abstract]
- Am J Transl Res. 2019 Apr 15;11(4):2155-2167. [Abstract]
- bioRxiv. 2026 Jun 26.
- bioRxiv. 2026 Jun 12.
- Technical University of Dresden. 2025.
- Res Sq. 2025 Apr 18.
- bioRxiv. 2025 February 27.
- bioRxiv. 2024 Nov 30:2024.11.29.626099. [Abstract]
- Heidelberg University. 2024.
- Wright State University. 2023 Feb 23.
- Research Square Preprint. 2021 Sep.
- University of Toyama. 2019 May.
Customer Validation & Images
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Biological Activity
Ki: 38 nM (TβRI), 300 nM (TβRII)
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Cell Line
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Type | Value | Description | References |
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| Calu-6 | EC50 |
0.236 μM
Compound: 15d
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Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay
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[PMID: 18314943] |
| NIH3T3 | IC50 |
0.21 μM
Compound: 15d
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Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
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[PMID: 18314943] |
| Sf9 | IC50 |
0.069 μM
Compound: 15d
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Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
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[PMID: 18314943] |
LY2109761 significantly inhibits the growth of L3.6pl/GLT soft agar colonies in a dose-dependent manner, and results in appr 33% inhibition at 2 μM and 73% inhibition at 20 μM. Targeting TβRI/II kinase activity with LY2109761 (5 μM) almost completely suppresses both the basal and TGF-β1-stimulated migration of L3.6pl/GLT cells[1].
LY2109761 induces a dose-dependent reduction in phosphorylation of Smad-2. HLE endogenous phosphorylation of Smad-2 is inhibited by LY2109761. LY2109761 blocks migration on different ECM proteins and invasion of both HLE and HLF through a 3-dimensional structure. LY2109761 increases E-cadherin mRNA expression after 24 hours and protein levels after 48 hours[2].
LY2109761 pretreatment reduces clonogenic survival in cell cultures of U87MG and T98 following radiation, resulting in an increase in the radiosensitivity with a DEF0.1 of 1.30 and 1.37, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LY2109761 enhances radiation-induced tumor growth delay in a U87MG subcutaneous xenograft tumor model in BALB/c nude mice. LY2109761 increases survival in an orthotopical CSLC glioblastoma model and enhanced antitumor activity of radiation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 700874-71-1
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Appearance Solid
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Molecular Weight 441.52
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Formula C26H27N5O2
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Color White to yellow
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SMILES
N12N=C(C(C3=C4C=CC(OCCN5CCOCC5)=CC4=NC=C3)=C1CCC2)C6=NC=CC=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (71)
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Journal Impact Factor
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Most Recent
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J Hepatol
EDIL3 is a novel regulator of epithelial-mesenchymal transition controlling early recurrence of hepatocellular carcinoma. [Abstract]2015 Oct;63(4):863-73. PMID: 25980764
LY2109761 purchased from MedChemExpress. Usage Cited in: J Hepatol. 2015 Oct;63(4):863-73. [Abstract]
Blocking the TGF-beta and ERK signalling effectively inhibits EDIL3 mediated angiogenesis and invasion. Western blotting analysis of the expression of p-ERK and p-Smad2 in DMSO- and VX-11e or LY2109761-treated HuH7-p-lenti-EDIL3 cells. GAPDH is used as a loading control.
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Cell Res
Transdifferentiation of tumor infiltrating innate lymphoid cells during progression of colorectal cancer. [Abstract]2020 Jul;30(7):610-622. PMID: 32367039 -
Hepatology
KIAA1199 drives immune suppression to promote colorectal cancer liver metastasis by modulating neutrophil infiltration. [Abstract]2022 Oct;76(4):967-981. PMID: 35108400 -
Nat Commun
2025 Sep 10;16(1):8049. PMID: 40931030 -
Nat Commun
CD206+ M2-like macrophages regulate systemic glucose metabolism by inhibiting proliferation of adipocyte progenitors. [Abstract]2017 Aug 18;8(1):286. PMID: 28819169 -
Sci Transl Med
Selective inhibition of TGFβ1 activation overcomes primary resistance to checkpoint blockade therapy by altering tumor immune landscape. [Abstract]2020 Mar 25;12(536):eaay8456. PMID: 32213632 -
J Exp Clin Cancer Res
Irradiation induces DJ-1 secretion from esophageal squamous cell carcinoma cells to accelerate metastasis of bystander cells via a TGF-β1 positive feedback loop. [Abstract]2022 Aug 26;41(1):259. PMID: 36008860 -
Int J Biol Sci
Cathelicidin-related antimicrobial peptide protects against cardiac fibrosis in diabetic mice heart by regulating endothelial-mesenchymal transition. [Abstract]2019 Sep 7;15(11):2393-2407. PMID: 31595157 -
Cell Commun Signal
Secreted RCN3 acts as an early epithelial-fibroblast mediator via TGFβR1-Smad signaling in post-ALI pulmonary fibrosis. [Abstract]2026 Feb 9;24(1):167. PMID: 41664195 -
Int J Biol Macromol
Angiopoietin-like protein 6 protects against methionine-choline deficient diet induced liver fibrosis by suppressing hepatic stellate cells activation via TGF-β1/Smad3 pathway. [Abstract]2026 Apr:356:151571. PMID: 41864387 -
Acta Pharmacol Sin
N-n-Butyl haloperidol iodide ameliorates liver fibrosis and hepatic stellate cell activation in mice. [Abstract]2022 Jan;43(1):133-145. PMID: 33758354 -
Sci Total Environ
Endosulfan triggers epithelial-mesenchymal transition via PTP4A3-mediated TGF-β signaling pathway in prostate cancer cells. [Abstract]2020 Aug 20;731:139234. PMID: 32413665 -
J Transl Med
Knockdown of eIF3a alleviates pulmonary arterial hypertension by inhibiting endothelial-to-mesenchymal transition via TGFβ1/SMAD pathway. [Abstract]2025 May 9;23(1):524. PMID: 40346622 -
Biomed Pharmacother
The CD73 is induced by TGF-β1 triggered by nutrient deprivation and highly expressed in dedifferentiated human melanoma. [Abstract]2023 Sep:165:115225. PMID: 37517292 -
Biomed Pharmacother
Bone marrow mesenchymal stem cells in microenvironment transform into cancer-associated fibroblasts to promote the progression of B-cell acute lymphoblastic leukemia. [Abstract]2020 Oct:130:110610. PMID: 34321159 -
Cell Death Discov
METTL3-m6A-mediated TGF-β signaling promotes Fuchs endothelial corneal dystrophy via regulating corneal endothelial-to-mesenchymal transition. [Abstract]2025 Mar 15;11(1):104. PMID: 40089501 -
Cell Death Discov
Circ_0020256 induces fibroblast activation to drive cholangiocarcinoma development via recruitment of EIF4A3 protein to stabilize KLF4 mRNA. [Abstract]2023 May 13;9(1):161. PMID: 37179359 -
Cell Rep
Immunosuppressive myeloid cells induce mesenchymal-like breast cancer stem cells by a membrane-bound TGF-β1-dependent mechanism. [Abstract]2026 Jun 18;45(7):117568. PMID: 42319830 -
Cell Rep
Regulatory T cell-derived TGF-β signaling governs the differentiation and maintenance of tumor-infiltrating bystander CD8+ T cells. [Abstract]2026 Mar 27;45(4):117189. PMID: 41903139 -
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J Biol Eng
Enhancing the therapeutic efficacy of gemcitabine in bladder cancer through TGF-β1 inhibition and pluronic F-127-based microsphere delivery. [Abstract]2025 Jul 11;19(1):62. PMID: 40646590 -
Phytother Res
Loureirin B Accelerates Diabetic Wound Healing by Promoting TGFβ/Smad-Dependent Macrophage M2 Polarization: A Concerted Analytical Approach Through Single-Cell RNA Sequencing and Experimental Verification. [Abstract]2024 Nov 12. PMID: 39532388 -
JCI Insight
Injury-induced FoxM1 expression in mouse kidney drives epithelial proliferation by a Cyclin F dependent mechanism. [Abstract]2024 Jun 25:e175416. PMID: 38916959 -
Ecotoxicol Environ Saf
Di-n-butyl phthalate induces oversecretion of vascular endothelium-derived NAP-2 and promotes epithelial-mesenchymal transition of urothelial cells in newborn hypospadias rats. [Abstract]2023 May:256:114892. PMID: 37059017 -
Ecotoxicol Environ Saf
Endosulfan promotes cell proliferation and extracellular matrix accumulation through TGF-β/Smad signaling pathway in HRMCs. [Abstract]2021 Nov 30:228:113040. PMID: 34856488 -
J Dent Res
2019 Jul;98(8):896-903. PMID: 31189369 -
Int J Mol Med
Osteocyte TGFβ1‑Smad2/3 is positively associated with bone turnover parameters in subchondral bone of advanced osteoarthritis. [Abstract]2020 Jul;46(1):167-178. PMID: 32319543 -
Int J Mol Med
AST IV inhibits H₂O₂-induced human umbilical vein endothelial cell apoptosis by suppressing Nox4 expression through the TGF-β1/Smad2 pathway. [Abstract]2015 Jun;35(6):1667-74. PMID: 25891879
LY2109761 purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2015 Jun;35(6):1667-74. [Abstract]
Inhibition of the TGF-β1/Smad2 pathway decreases H2O2-induced human umbilical vein endothelial cell (HUVEC) apoptosis, but not oxidative stress. Western blot analysis is performed to determine protein expression in the HUVECs in the control, model, AST Ⅳ and LY2109761 groups.
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Cell Prolif
Cellular senescence mediates retinal ganglion cell survival regulation post-optic nerve crush injury. [Abstract]2024 Jul 18:e13719. PMID: 39021340 -
Biochem Pharmacol
Modulation of epithelial-mesenchymal transition by gemcitabine: Targeting ionizing radiation-induced cellular senescence in lung cancer cell. [Abstract]2024 Jun:224:116234. PMID: 38670436 -
Biochem Pharmacol
Upregulation of IL-37 in epithelial cells: A potential new mechanism of T cell inhibition induced by tacrolimus. [Abstract]2023 Oct:216:115796. PMID: 37690572 -
Life Sci
Esaxerenone inhibits renal macrophage proliferation through MR/TGF-β1 pathway in db/db mice. [Abstract]2025 Oct 9:382:124008. PMID: 41067301 -
Life Sci
Bone mesenchymal stem cells promote gastric cancer progression through TGF-β1/Smad2 positive feedback loop. [Abstract]2023 Jun 15:323:121657. PMID: 37019301 -
Int J Mol Sci
Mechanism of THBS1 Regulation of MDCK Cell Proliferation and Apoptosis Through TGF-β/Smad Signalling. [Abstract]2025 Jan 4;26(1):395. PMID: 39796249 -
Int J Mol Sci
Esaxerenone Inhibits Renal Angiogenesis and Endothelial-Mesenchymal Transition via the VEGFA and TGF-β1 Pathways in Aldosterone-Infused Mice. [Abstract]2023 Jul 21;24(14):11766. PMID: 37511521 -
Am J Physiol Cell Physiol
Ablation of tumor-derived IGFBP-3 attenuates cancer-associated skeletal muscle wasting in murine pancreatic cancer. [Abstract]2026 Feb 1;330(2):C467-C481. PMID: 41525104 -
Int Immunopharmacol
Eplerenone inhibits the macrophage-to-myofibroblast transition in rats with UUO-induced type 4 cardiorenal syndrome through the MR/CTGF pathway. [Abstract]2022 Dec;113(Pt A):109396. PMID: 36461595 -
Invest Ophthalmol Vis Sci
Activated Blood Coagulation Factor X (FXa) Contributes to the Development of Traumatic PVR Through Promoting RPE Epithelial-Mesenchymal Transition. [Abstract]2021 Jul 1;62(9):29. PMID: 34283209 -
Int Immunopharmacol
Destruction of the blood-retina barrier in diabetic retinopathy depends on angiotensin-converting enzyme-mediated TGF-β1/Smad signaling pathway activation. [Abstract]2020 Aug;85:106686. PMID: 32531714 -
Mol Nutr Food Res
Novel Calcium-Binding Peptide from Bovine Bone Collagen Hydrolysates and Its Potential Pro-Osteogenic Activity via Calcium-Sensing Receptor (CaSR). [Abstract]2024 Feb;68(4):e2200726. PMID: 38161238 -
J Cell Mol Med
Pirfenidone inhibits TGF-β1-induced metabolic reprogramming during epithelial-mesenchymal transition in non-small cell lung cancer. [Abstract]2024 Feb;28(3):e18059. PMID: 38140828 -
J Cell Mol Med
TGF-β isoforms inhibit hepatitis C virus propagation in transforming growth factor beta/SMAD protein signalling pathway dependent and independent manners. [Abstract]2021 Apr;25(7):3498-3510. PMID: 33682288 -
FEBS J
Dramatically changed immune-related molecules as early diagnostic biomarkers of non-small cell lung cancer. [Abstract]2020 Feb;287(4):783-799. PMID: 31482685 -
Biochim Biophys Acta Mol Basis Dis
Sphingosine kinase 2 cooperating with Fyn promotes kidney fibroblast activation and fibrosis via STAT3 and AKT. [Abstract]2018 Nov;1864(11):3824-3836. PMID: 30251698
LY2109761 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. [Abstract]
LY2109761 at 100 nM, 10 μM, or 50 μM is added for 30 min to block TGFβR1/2 prior to TGF-β1-treatment, then proteins are collected, and the levels of Sphk2, fibronectin, and α-SMA are detected by Western blotting.
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J Inherit Metab Dis
Transforming Growth Factor-β-Mediated Fibrotic Remodeling Drives Chronic Kidney Disease in Methylmalonic Aciduria and Propionic Aciduria-Identification of a New Therapeutic Target. [Abstract]2025 Nov;48(6):e70111. PMID: 41137992 -
J Virol
Rabies virus utilizes neuropilin 2 as an endocytic receptor to trigger TGFBR1-mediated actin polymerization. [Abstract]2025 Jun 25:e0063825. PMID: 40558096 -
Mol Cell Biochem
WISP1 promotes bovine MDSC differentiation via recruitment of ANXA1 for the regulation of the TGF-β signalling pathway. [Abstract]2020 Jul;470(1-2):215-227. PMID: 32458119 -
Mol Cell Biochem
Knockdown of KDM2A inhibits proliferation associated with TGF-β expression in HEK293T cell. [Abstract]2019 Jun;456(1-2):95-104. PMID: 30604066 -
Am J Pathol
2023 Aug;193(8):1029-1045. PMID: 37236504 -
Int J Med Sci
Modulation of Chemotherapy Sensitivity of Breast Cancer Cells through Transforming Growth Factor-beta Pathway-mediated Alterations in DNA Damage Response. [Abstract]2025 Mar 31;22(9):2031-2039. PMID: 40303493 -
Pathol Res Pract
2025 Mar 23:269:155899. PMID: 40168772 -
Front Biosci (Landmark Ed)
Aldosterone-Induced Renal Lymphangiogenesis and Endothelial-To-Mesenchymal Transformation to Promote Renal Interstitial Fibrosis Through the MR/TGF-β1 Pathway in Mice. [Abstract]2025 Nov 27;30(11):45591. PMID: 41351406 -
Front Biosci (Landmark Ed)
β-Adrenoceptor Signaling Activation Improves Bladder Fibrosis by Inhibiting Extracellular Matrix Deposition of Bladder Outlet Obstruction. [Abstract]2024 Sep 24;29(9):336. PMID: 39344310 -
Cell Biol Int
2017 Sep;41(9):960-968. PMID: 28493530
LY2109761 purchased from MedChemExpress. Usage Cited in: Cell Biol Int. 2017 Sep;41(9):960-968. [Abstract]
The phosphorylation level of Smad2 is significantly inhibited by LY2109761. The M2 macrophage-induced increase of α-SMA and decrease of E-cadherin and CK-18 are inhibited by LY2109761.
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Mol Immunol
TGF-β1-Induced Airway Smooth Muscle Cell Proliferation Involves TRPM7-Dependent Calcium Influx via TGFβR/SMAD3. [Abstract]2018 Nov:103:173-181. PMID: 30290314
LY2109761 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2018 Nov:103:173-181. [Abstract]
TRPM7 mRNA and protein expressions are effectively suppressed by LY2109761 and SIS3 in ASMCs compared with those in 10 ng/mL TGF-β1-stimulated cells.
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Brain Sci
Astrocyte-Derived TGFβ1 Facilitates Blood-Brain Barrier Function via Non-Canonical Hedgehog Signaling in Brain Microvascular Endothelial Cells. [Abstract]2021 Jan 8;11(1):77. PMID: 33430164 -
J Cell Biochem
β-Adrenoceptor signaling regulates proliferation and contraction of human bladder smooth muscle cells under pathological hydrostatic pressure. [Abstract]2019 Oct;120(10):17872-17886. PMID: 31161623 -
Photochem Photobiol
Compound collagen peptide powder improves skin photoaging by reducing oxidative stress and activating TGF-β1/Smad pathway. [Abstract]2024 Nov-Dec;100(6):1874-1893. PMID: 38504445 -
Exp Ther Med
Procyanidin B2 suppresses hyperglycemia-induced renal mesangial cell dysfunction by modulating CAV-1-dependent signaling. [Abstract]2022 Jun 7;24(2):496. PMID: 35837062 -
Exp Ther Med
Role of TGF-β1-mediated epithelial-mesenchymal transition in the pathogenesis of tympanosclerosis. [Abstract]2021 Jan;21(1):6. PMID: 33235615 -
Am J Transl Res
Blocking transforming growth factor-beta reduces the migration and invasion of the residual tumour after TAE. [Abstract]2019 Apr 15;11(4):2155-2167. PMID: 31105825 -
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bioRxiv
Dysregulated RNA splicing induces regeneration failure in alcohol-associated liver disease. [Abstract]2024 Nov 30:2024.11.29.626099. PMID: 39651310 -
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Solvent & Solubility
DMSO : 6.67 mg/mL (15.11 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Protocol
L3.6pl/GLT cells are washed twice with cold PBS and lysed at 4°C into RIPA buffer (50 mM Tris HCl [pH 8], 150 mM NaCl, 1% NP-40, 0.5% sodium deoxycolate, and 0.1% SDS). Tumor and liver specimens are homogenized into RIPA buffer with an electric homogenizer and then maintained in constant agitation for two hours at 4°C. The lysates are cleared by centrifugation. Each lysate (20 µg of protein) is separated by 8% SDS-PAGE and probed with polyclonal rabbit antibodies against total ERK1/2, TβRI, and TβRII or with monoclonal mouse antibodies against phosphorylated Smad2, total Smad2, phosphorylated ERK1/2, and phosphorylated and total JNK. Immunoreactive proteins are visualized with Lumi-Light Western blotting substrate according to the manufacturer's instructions. phosphorylated Smad2/Smad2 band density ratios are calculated using the ImageQuant software.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fifty mice are randomLy allocated into five groups (n=5 mice per group) to receive p.o. vehicle for 50 μL of LY2109761 or 50 mg/kg LY2109761 twice a day p.o. On day 0, mice are anesthetized with 1.5% isofluorane-air mixture, a small left abdominal flank incision is created, and the spleen is carefully exteriorized. L3.6pl/GLT or C5LM2/GLT cells (1.0×105 cells/50 μL of HBSS), cultured in the presence of LY2109761 (5 μM) or DMSO from day −5 to day 0, are inoculated into the spleen with a 30-gauge needle. A visible paling of the spleen is the criterion for successful inoculation. After 10 min, the spleen is removed using a high-temperature cautery to avoid the possibility that the ectopic growth of pancreatic tumor cells in the spleen could be a confounding source of hematogenous liver metastatic cells. The abdominal wall is closed in one layer with wound clips. Treatment with 50 mg/kg LY2109761 twice a day p.o. (days 1-5 of each week after inoculation) is continued for one group of untreated mice inoculated with untreated cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Melisi D, et al. LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol Cancer Ther, 2008, 7(4), 829-840. [Content Brief]
[2]. Fransvea E, et al. Blocking transforming growth factor-beta up-regulates E-cadherin and reduces migration and invasion of hepatocellular carcinoma cells. Hepatology, 2008, 47(5), 1557-1566. [Content Brief]
[3]. Zhang M, et al. Blockade of TGF-β signaling by the TGFβR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res, 2011, 71(23), 7155-7167. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2649 mL | 11.3245 mL | 22.6490 mL | 56.6226 mL |
| 5 mM | 0.4530 mL | 2.2649 mL | 4.5298 mL | 11.3245 mL | |
| 10 mM | 0.2265 mL | 1.1325 mL | 2.2649 mL | 5.6623 mL | |
| 15 mM | 0.1510 mL | 0.7550 mL | 1.5099 mL | 3.7748 mL |
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