PDGFRβ
PDGFRβ is a cell-surface receptor tyrosine kinase that organizes PDGF-B/PDGFRβ signaling in vascular mural cells[1]. Mechanistically, ligand binding drives PDGFRβ dimerization and autophosphorylation, creating docking sites for SH2-domain signaling proteins that regulate proliferation, migration, matrix deposition, and early gene induction[2]. In mouse embryonic vessels, endothelial PDGF-B recruits PDGFRβ-positive vascular smooth muscle cells/pericytes, supporting vessel growth and mural-cell coverage[1]. In adult mouse brain, PDGFRβ expression is restricted to pericytes rather than neurons, astrocytes, or endothelial cells, making it useful for pericyte-focused experimental models[3]. Compared with PDGFRα, PDGFRβ shows distinct ligand preference because PDGF-D activates PDGFRβ but not PDGFRα in cells expressing individual receptors[4]. For experimental applications, imatinib and crenolanib inhibit PDGF-induced PDGFR autophosphorylation, enabling pathway-blockade studies in PDGFRB-dependent cellular models[5].
References:
- [1]. Hellström M, et al. Role of PDGF-B and PDGFR-beta in recruitment of vascular smooth muscle cells and pericytes during embryonic blood vessel formation in the mouse. Development. 1999 Jun;126(14):3047-55. [Content Brief]
- [2]. Tallquist MD, et al. Additive effects of PDGF receptor beta signaling pathways in vascular smooth muscle cell development. PLoS Biol. 2003 Nov;1(2):E52. [Content Brief]
- [3]. Winkler EA, et al. Pericyte-specific expression of PDGF beta receptor in mouse models with normal and deficient PDGF beta receptor signaling. Mol Neurodegener. 2010 Aug 25;5:32. [Content Brief]
- [4]. Bergsten E, et al. PDGF-D is a specific, protease-activated ligand for the PDGF beta-receptor. Nat Cell Biol. 2001 May;3(5):512-6. [Content Brief]
- [5]. Melaiu O, et al. Inhibition of the platelet-derived growth factor receptor beta (PDGFRB) using gene silencing, crenolanib besylate, or imatinib mesylate hampers the malignant phenotype of mesothelioma cell lines. Genes Cancer. 2017 Jan;8(1-2):438-452. [Content Brief]
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PDGFRβ Related Products (93)
Related Products (93)
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Recombinant Proteins (10)
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Antibodies (1)
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LY2457546
0 ImagesCat. No.: HY-107144CAS No.: 908265-94-1LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.
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Multi-kinase-IN-2
0 ImagesCat. No.: HY-150026CAS No.: 2095628-21-8Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
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Multi-kinase-IN-3
0 ImagesCat. No.: HY-150027CAS No.: 2091950-43-3Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively.
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pPB peptide
0 ImagesCat. No.: HY-P11549CAS No.: 663933-94-6pPB peptide is a cyclic peptide targeting platelet-derived growth factor receptor β (PDGFRβ). Derived from natural platelet-derived growth factor (PDGF), pPB peptide contains arginine and isoleucine as key receptor-binding residues. pPB peptide specifically binds to PDGFRβ, which is highly expressed on the surface of activated hepatic stellate cells (HSC). pPB peptide can be used in studies related to liver fibrosis, liver cirrhosis, and tumor-specific drug delivery.
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VEGFR2-IN-84
0 ImagesCat. No.: HY-182354CAS No.: 861877-12-5VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors.
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VEGFR-2-IN-89
0 ImagesCat. No.: HY-184720VEGFR-2-IN-89 is a VEGFR-2 inhibitor with an IC50 of 77 nM. VEGFR-2-IN-89 potently inhibits c-Met kinase activity with an IC50 of 0.152 μM, and also exhibits good inhibitory activity against EGFR (IC50 = 0.269 μM) and PDGFR-β kinase (IC50 = 0.301 μM). VEGFR-2-IN-89 displays anticancer activity against liver cancer. VEGFR-2-IN-89 can be used in the research of hepatocellular carcinoma.
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IHMT-TRK-284
0 ImagesCat. No.: HY-146697CAS No.: 2416844-79-4
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Henatinib
0 ImagesCat. No.: HY-13645CAS No.: 1239269-51-2Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs).
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KBP-7018
0 ImagesCat. No.: HY-117873CAS No.: 1613437-66-3KBP-7018 is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC50 value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 can be used in research related to idiopathic pulmonary fibrosis.
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TG 100801 Hydrochloride
0 ImagesCat. No.: HY-10187CAS No.: 1018069-81-2TG 100801 Hydrochloride is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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N-(p-Coumaroyl) Serotonin (Standard)
0 ImagesCat. No.: HY-129440RCAS No.: 68573-24-0N-(p-Coumaroyl) Serotonin (Standard) is the analytical standard of N-(p-Coumaroyl) Serotonin (HY-129440). This product is intended for research and analytical applications. N-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.
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VEGFR-2-IN-44
0 ImagesCat. No.: HY-112337CAS No.: 288144-20-7VEGFR-2-IN-44 (compound 4b) is a selective VEGF-R2 (Flk-1) inhibitor with an IC50 value of 70 nM. VEGFR-2-IN-44 also inhibits PDGF-Rβ with an IC50 of 920 nM.
