Date published: 2025-11-22

1-800-457-3801

SCBT Portrait Logo
Seach Input

LY2109761 (CAS 700874-71-1)

5.0(1)
Write a reviewAsk a question

See product citations (9)

Alternate Names:
4-[5,6-dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline
Application:
LY2109761 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases
CAS Number:
700874-71-1
Purity:
≥98%
Molecular Weight:
441.52
Molecular Formula:
C26H27N5O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

QUICK LINKS

LY2109761 is a chemical compound utilized in the field of biochemistry and cell biology for its role as an inhibitor of transforming growth factor-beta (TGF-β) receptor kinases. This inhibition is of interest in studies investigating the signaling pathways that influence cell proliferation, differentiation, and migration. LY2109761 helps identify the complex processes of cellular communication and regulation by selectively targeting and modulating the TGF-β pathway. The compound′s mechanism of action involves the prevention of phosphorylation events that are typically induced by TGF-β, thereby modulating downstream effects. LY2109761 is utilized in dissecting the TGF-β signaling cascade and for exploring the molecular mechanisms underlying various biological responses to TGF-β. It is also in studies that examine the role of TGF-β signaling tissue homeostasis.


LY2109761 (CAS 700874-71-1) References

  1. Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.  |  Li, HY., et al. 2008. J Med Chem. 51: 2302-6. PMID: 18314943
  2. LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis.  |  Melisi, D., et al. 2008. Mol Cancer Ther. 7: 829-40. PMID: 18413796
  3. Dual-responsive nanosystem based on TGF-β blockade and immunogenic chemotherapy for effective chemoimmunotherapy.  |  Huang, X., et al. 2022. Drug Deliv. 29: 1358-1369. PMID: 35506467
  4. TGF-β-Induced FLRT3 Attenuation Is Essential for Cancer-Associated Fibroblast-Mediated Epithelial-Mesenchymal Transition in Colorectal Cancer.  |  Yang, M., et al. 2022. Mol Cancer Res. 20: 1247-1259. PMID: 35560224
  5. Dietary intake of GDF11 delays the onset of several biomarkers of aging in male mice through anti-oxidant system via Smad2/3 pathway.  |  Song, L., et al. 2022. Biogerontology. 23: 341-362. PMID: 35604508
  6. Effect of ALA-PDT on inhibition of oral precancerous cell growth and its related mechanisms.  |  Jin, JQ., et al. 2022. Lasers Med Sci. 37: 3461-3472. PMID: 35796919
  7. Puerarin protects fibroblasts against mechanical stretching injury through Nrf2/TGF-β1 signaling pathway.  |  Li, Y., et al. 2022. Int Urogynecol J. 33: 2565-2576. PMID: 35962806
  8. Salidroside alleviates dexamethasone-induced inhibition of bone formation via transforming growth factor-beta/Smad2/3 signaling pathway.  |  Xie, B., et al. 2023. Phytother Res. 37: 1938-1950. PMID: 36567454
  9. Subclonal evolution and expansion of spatially distinct THY1-positive cells is associated with recurrence in glioblastoma.  |  Al-Holou, WN., et al. 2023. Neoplasia. 36: 100872. PMID: 36621024
  10. Pirfenidone suppressed triple-negative breast cancer metastasis by inhibiting the activity of the TGF-β/SMAD pathway.  |  Luo, D., et al. 2023. J Cell Mol Med. 27: 456-469. PMID: 36651490
  11. Gallium-modified gelatin nanoparticles loaded with quercetin promote skin wound healing via the regulation of bacterial proliferation and macrophage polarization.  |  Yang, N., et al. 2023. Front Bioeng Biotechnol. 11: 1124944. PMID: 36777248
  12. An immune and epithelial-mesenchymal transition-related risk model and immunotherapy strategy for grade II and III gliomas.  |  Luo, W., et al. 2022. Front Genet. 13: 1070630. PMID: 36778912
  13. FUT1-mediated terminal fucosylation acts as a new target to attenuate renal fibrosis.  |  Luo, J., et al. 2023. Mol Med. 29: 55. PMID: 37085770
  14. Dual Blockade of TGF-β Receptor and Endothelin Receptor Synergistically Inhibits Angiotensin II-Induced Myofibroblast Differentiation: Role of AT1R/Gαq-Mediated TGF-β1 and ET-1 Signaling.  |  Duangrat, R., et al. 2023. Int J Mol Sci. 24: PMID: 37108136
  15. Circ_0020256 induces fibroblast activation to drive cholangiocarcinoma development via recruitment of EIF4A3 protein to stabilize KLF4 mRNA.  |  Li, Z., et al. 2023. Cell Death Discov. 9: 161. PMID: 37179359
  16. Crosstalk between the JAK2 and TGF-β1 signaling pathways in scleroderma-related interstitial lung disease targeted by baricitinib.  |  Wang, D., et al. 2023. Adv Rheumatol. 63: 22. PMID: 37194022

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

LY2109761, 1 mg

sc-396262
1 mg
$87.00

LY2109761, 5 mg

sc-396262A
5 mg
$270.00

What is the unit for molecular weight of this compound?

Asked by: Chaitrali
Thank you for your question. The molecular weight for this compound is ~440. You can see a sample CoA here: http://datasheets.scbt.com/coa/coa.php?sc=sc-396262A&lot=F0418
Answered by: Tech Service
Date published: 2019-03-20

Is there any protein binding property of the compound?

Asked by: T Luang
Thank you for your question. sc-396262 (LY2109761) is dual inhibitor of both TGF-β receptor type I/II (TβRI/II), with Ki of 38 nM and 300 nM in a cell-free assay, respectively. Melisi D, Ishiyama S, Sclabas GM 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: 829-840. PMID: 18413796
Answered by: Technical Support
Date published: 2017-08-18

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. This chemical is supplied as a light brown powder. Please contact Technical Service if you have further questions concerning this product.
Answered by: Tech Service 9
Date published: 2017-01-14

Is this stable in solution?  Can a stocking solution be made?

Asked by: two2igm05
Thank you for you question. LY2109761, sc-396262, can be made into a stocking solution. We recommended that stock solutions, once prepared, are stored as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Wherever possible, solutions should be made up and used as soon as possible. It is soluble in DMSO at 2 mg/mL (4.52 mM), Water at <1 mg/mL, and Ethanol at <1 mg/mL.
Answered by: TechService7
Date published: 2016-12-15
  • y_2025, m_11, d_12, h_6CST
  • bvseo_bulk, prod_bvqa, vn_bulk_3.0.42
  • cp_1, bvpage1
  • co_hasquestionsanswers, tq_4
  • loc_en_US, sid_396262, prod, sort_[SortEntry(order=LAST_APPROVED_ANSWER_SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-4.0.0
  • CLOUD, getContent, 104ms
  • QUESTIONS, PRODUCT
Rated 5 out of 5 by from Ren et alRen et al. (PubMed ID 25912577) found that LY2109761 inhibited metastasis and enhanced chemosensitivity in osteosarcoma MG-63 cells by attenuating S100A4 expression. -SCBT Publication Review
Date published: 2015-04-13
  • y_2025, m_11, d_12, h_6
  • bvseo_bulk, prod_bvrr, vn_bulk_3.0.42
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_396262, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-4.0.0
  • CLOUD, getReviews, 14ms
  • REVIEWS, PRODUCT
LY2109761 is rated 5.0 out of 5 by 1.
  • y_2025, m_11, d_12, h_6
  • bvseo_bulk, prod_bvrr, vn_bulk_3.0.42
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_396262, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-4.0.0
  • CLOUD, getAggregateRating, 109ms
  • REVIEWS, PRODUCT