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]
All Product Categories
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PDGFRβ 관련 제품 (90)
관련 제품 (90)
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Recombinant Proteins (10)
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Antibodies (1)
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Lenvatinib
0 ImagesSynonyms: E7080
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Nintedanib
0 ImagesSynonyms: BIBF 1120Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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Sunitinib
0 ImagesSynonyms: SU 11248Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
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Regorafenib
0 ImagesSynonyms: BAY 73-4506
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GW296115
0 ImagesCat. No.: HY-186224CAS No.: 118458-58-5GW296115 is a multi-target inhibitor with the following IC50 values against its targets: 8.4 nM for BRSK2, 21 nM for BRSK1, 1.8 μM for PDGFRβ, 5.5 nM for STK17B/DRAK2, 28 nM for DRAK1, 20 nM for PHKG1, and 89 nM for DCAMKL3. GW296115 downregulates the phosphorylation of S317 site on ULK1 and S351 site on P62, which are AMPK substrates driven by BRSK2. GW296115 does not alter the phosphorylation level of AMPK at T172, reduces nutrient deprivation-mediated Autophagy and autophagosome formation, and enhances Apoptosis. GW296115 exhibits anticancer activity against triple-negative breast cancer. GW296115 is applicable for breast cancer-related research.
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BRD4-IN-41
0 ImagesCat. No.: HY-115541CAS No.: 1877286-69-5BRD4-IN-41 is a BRD4 inhibitor with an IC50 of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.
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VEGFR/PDGFR/CA II-IN-1
0 ImagesCat. No.: HY-184656CAS No.: 3099422-14-4VEGFR/PDGFR/CA II-IN-1 is a VEGFR/PDGFR/CA II inhibitor. VEGFR/PDGFR/CA II-IN-1 potently inhibits VEGFR2 (IC50 = 62.66 nM), PDGFRα (IC50 = 18.65 nM), PDGFRβ (IC50 = 5.23 nM), and hCA II (Ki = 19.4 nM), with weaker activity against hCA I (Ki = 154.2 nM) and hCA IX (Ki = 121.0 nM). VEGFR/PDGFR/CA II-IN-1 exhibits potent antiproliferative activity in VEGFR2-BAF3 cells and robust inhibition of angiogenesis in human umbilical vein endothelial cells (HUVECs). VEGFR/PDGFR/CA II-IN-1 inhibits the formation of corneal neovascularization in rabbits through multiple signaling pathways, and significantly reduced intraocular pressure (IOP) in both acute and chronic glaucoma models. VEGFR/PDGFR/CA II-IN-1 can be used to study neovascular glaucoma (NVG).
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Nintedanib esylate
0 ImagesSynonyms: BIBF 1120 esylateNintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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Lenvatinib mesylate
0 ImagesSynonyms: E7080 mesylate
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Crenolanib
0 ImagesSynonyms: CP-868596Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
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Sunitinib Malate
0 ImagesSynonyms: SU 11248 MalateSunitinib (SU 11248) Malat is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malat, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
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Linifanib
0 ImagesSynonyms: ABT-869; AL-39324Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
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Velzatinib
0 ImagesSynonyms: M4205; IDRX-42
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Regorafenib monohydrate
0 ImagesSynonyms: BAY 73-4506 monohydrateRegorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
