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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TG 100801
0 ImagesTG 100801 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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Rinucumab
0 ImagesSynonyms: REGN 2176Rinucumab (REGN 2176) is an anti-PDGFR-β antibody. Rinucumab is used for research on neovascular age-related macular degeneration.
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Dovitinib lactate
0 ImagesSynonyms: CHIR-258 lactate; TKI-258 lactate
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Ilorasertib hydrochloride
0 ImagesSynonyms: ABT-348 hydrochlorideIlorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
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NVP-ACC789
0 ImagesSynonyms: ACC-789; ZK202650
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Flumatinib mesylate
0 ImagesSynonyms: HHGV678 mesylateFlumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model.
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N-Feruloylserotonin
0 ImagesSynonyms: (E/Z)-MoschamineN-Feruloylserotonin ((E/Z)-Moschamine) is a serotonin hydroxycinnamic acid amide. It can be isolated from a variety of plants, particularly the seeds of safflower (Carthamus tinctorius L.). N-Feruloylserotonin inhibits KCl- and 5-HT-induced elevation of intracellular [Ca2+]i. It suppresses PDGF-BB-induced phosphorylation of PDGFRβ and ERK1/2. N-Feruloylserotonin exerts anti-inflammatory effects on aortic endothelial cells. It inhibits atherosclerotic plaque formation in apolipoprotein E-deficient mice.
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Hypothemycin
0 ImagesCat. No.: HY-107417CAS No.: 76958-67-3
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(Z)-Orantinib
0 ImagesSynonyms: (Z)-SU6668; (Z)-TSU-68
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GZD856 formic
0 ImagesCat. No.: HY-101489ACAS No.: 2804039-78-7GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Myricanol
0 ImagesCat. No.: HY-N3225CAS No.: 33606-81-4Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation.
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Tyrphostin AG1433
0 ImagesSynonyms: SU1433; AG1433
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WQ-C-401
0 ImagesWQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension.
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PD-089828
0 ImagesPD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
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Sunitinib glucuronate
0 ImagesCat. No.: HY-10255CCAS No.: 1818285-48-1Synonyms: SU 11248 glucuronateSunitinib (SU 11248) glucuronate is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib glucuronate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
