Molecular structure of TGF-β RI Kinase Inhibitor VIII, CAS Number: 356559-20-1
TGF-β RI Kinase Inhibitor VIII (CAS 356559-20-1)
See product citations (2)
Application:
TGF-β RI Kinase Inhibitor VIII is a potent ATP-competitive inhibitor against receptor TbR-I/ALK5
CAS Number:
356559-20-1
Purity:
>97%
Molecular Weight:
343.4
Molecular Formula:
C21H21N5
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
VEGFR Tyrosine Kinase Inhibitor III, KRN633 is a cell-permeable, reversible, ATP-competitive inhibitor of VEGFR kinase activity (IC50 = 170 nM, 160 nM, and 125 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively). Inhibits PDGFR-α and c-Kit at higher concentrations only (IC50 = 0.97 µM and 4.33 µM, respectivly) and inactive towards 17 other kinases (IC50 ≥ 10 µM). Shown to suppress VEGF-dependent, but not FGF-dependent, cellular signaling and cell proliferation. Although not cytotoxic to cancer cells, KRN633 exhibits excellent in vivo antitumor activity due to its inhibitory effects on vessel formation and vascular permeability.
TGF-β RI Kinase Inhibitor VIII (CAS 356559-20-1) References
- Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. | Grygielko, ET., et al. 2005. J Pharmacol Exp Ther. 313: 943-51. PMID: 15769863
- Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. | Higashiyama, H., et al. 2007. Exp Mol Pathol. 83: 39-46. PMID: 17274978
- Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. | Laping, NJ., et al. 2007. Clin Cancer Res. 13: 3087-99. PMID: 17505012
- Follistatin-like 1 attenuates differentiation and survival of erythroid cells through Smad2/3 signaling. | Wu, J., et al. 2015. Biochem Biophys Res Commun. 466: 711-6. PMID: 26365350
- Transforming growth factor-β mediates endothelial dysfunction in rats during high salt intake. | Feng, W., et al. 2015. Am J Physiol Renal Physiol. 309: F1018-25. PMID: 26447221
- A Novel High-Throughput 3D Screening System for EMT Inhibitors: A Pilot Screening Discovered the EMT Inhibitory Activity of CDK2 Inhibitor SU9516. | Arai, K., et al. 2016. PLoS One. 11: e0162394. PMID: 27622654
- The effect of Echinococcus granulosus on spleen cells and TGF-β expression in the peripheral blood of BALB/c mice. | Yin, S., et al. 2017. Parasite Immunol. 39: PMID: 28130828
- Small Molecular TGF-β1-Inhibitor-Loaded Electrospun Fibrous Scaffolds for Preventing Hypertrophic Scars. | Wang, L., et al. 2017. ACS Appl Mater Interfaces. 9: 32545-32553. PMID: 28875694
- Refinement of In Vitro Methods for Identification of Aldehyde Oxidase Substrates Reveals Metabolites of Kinase Inhibitors. | Dick, RA. 2018. Drug Metab Dispos. 46: 846-859. PMID: 29615437
- Transforming growth factor β mediates communication of co-cultured human nucleus pulposus cells and mesenchymal stem cells. | Lehmann, TP., et al. 2018. J Orthop Res. 36: 3023-3032. PMID: 29999195
- Nrf2 protects stellate cells from Smad-dependent cell activation. | Prestigiacomo, V. and Suter-Dick, L. 2018. PLoS One. 13: e0201044. PMID: 30028880
- A high content, phenotypic 'scar-in-a-jar' assay for rapid quantification of collagen fibrillogenesis using disease-derived pulmonary fibroblasts. | Good, RB., et al. 2019. BMC Biomed Eng. 1: 14. PMID: 32903343
- PM2.5-exposed hepatocytes induce hepatic stellate cells activation by releasing TGF-β1. | Leilei, L., et al. 2021. Biochem Biophys Res Commun. 569: 125-131. PMID: 34243068
Inhibitor of:
ACTR-IB, C230096C10Rik, COL1A1, DAF-1, dsg1α, Dynamin-like, EG243866, elastin, FHL-2, Fumarylacetoacetase, IFN-γ, Layilin, LRRC70, netrin-1, Olfr593, PAI-1, SCAI, Smad7, Smad8, TBCK, TGF beta Receptor, TGF beta RI, and TGFβ RII.Activator of:
Inhibin β-B, SnoN_SnoN2_SnoA, SPINT4, TGFβ RIII, TTK, and WFIKKN.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TGF-β RI Kinase Inhibitor VIII, 2 mg | sc-203295 | 2 mg | $100.00 |