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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Sunitinib-d10
0 ImagesSynonyms: SU 11248-d10Sunitinib-d10 (SU 11248-d10) is a deuterium labeled Sunitinib. Sunitinib 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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Dovitinib lactate hydrate
0 ImagesCat. No.: HY-B0062CAS No.: 915769-50-5Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate
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Regorafenib mesylate
0 ImagesCat. No.: HY-10331BCAS No.: 835621-08-4Synonyms: BAY 73-4506 mesylateRegorafenib (BAY 73-4506) mesylate 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 mesylate shows very robust antitumor and antiangiogenic activity.
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GZD856
0 ImagesCat. No.: HY-101489CAS No.: 1257628-64-0
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Famitinib malate
0 ImagesCat. No.: HY-108713ACAS No.: 1256377-67-9Synonyms: SHR1020 malateFamitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer.
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SU 5402 (GMP)
0 ImagesCat. No.: HY-10407GCAS No.: 215543-92-3SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
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Multi-kinase inhibitor 3
0 ImagesCat. No.: HY-168114CAS No.: 2648279-76-7Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity.
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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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PDGFRβ-IN-1
0 ImagesCat. No.: HY-187366PDGFRβ-IN-1 is an orally active PDGFRβ inhibitor with an IC50 of 3.9 nM against human PDGFRβ. PDGFRβ-IN-1 selectively inhibits PDGFRβ, blocks its downstream signaling pathways, and promotes its degradation via a non-classical pathway. PDGFRβ-IN-1 inhibits cancer cell proliferation, migration and colony formation, and induces cancer cell apoptosis. PDGFRβ-IN-1 suppresses tumor growth in xenograft models. PDGFRβ-IN-1 can be used for the research of hepatocellular carcinoma.
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Ki11502
0 ImagesKi11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.
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HSN748
0 ImagesCat. No.: HY-171146CAS No.: 2409925-53-5HSN748 is a Ponatinib (HY-12047) analogue and a multikinase inhibitor. HSN748 has inhibitory activity on FLT3, ABL1, RET, PDGFRα/β, MNK1, MNK2 and other kinases. HSN748 can inhibit the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines and can be used in the study of leukemia.
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Tyrosine kinase-IN-11
0 ImagesTyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor. Tyrosine kinase-IN-11 decreases general tyrosine kinase activity, selectively inhibits PDGFR-β, SRC, and c-MET kinases. Tyrosine kinase-IN-11 induces apoptosis, accompanied by reduced ERK signalings. Tyrosine kinase-IN-11 exhibits selective anticancer activity against pancreatic cancer and renal cancer.
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SA-PA
0 ImagesCat. No.: HY-155684CAS No.: 3058085-76-7SA-PA is an intracellular self-assembling CRBN-recruiting PROTAC composed of an alkynylated Sorafenib precursor (SA) and an azidated Pomalidomide precursor (PA). SA-PA promotes the ubiquitination and proteasomal degradation of VEGFR-2, EphB4, and PDGFR-β, and exhibits inhibitory activity against U87 and A549 cell proliferation. SA-PA is used in cancer-related research, such as glioblastoma and non-small cell lung cancer.
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JI-101 hydrochloride
0 ImagesCat. No.: HY-16265ACAS No.: 2514957-81-2JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity.JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis.JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes.JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route.JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors.
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KBP-7018 hydrochloride
0 ImagesCat. No.: HY-117873ACAS No.: 1613437-67-4KBP-7018 hydrochloride 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 hydrochloride improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 hydrochloride can be used in research related to idiopathic pulmonary fibrosis.
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VEGFR-2-IN-88
0 ImagesCat. No.: HY-184719VEGFR-2-IN-88 is a VEGFR-2 inhibitor with an IC50 of 0.202 μM. VEGFR-2-IN-88 potently inhibits EGFR (IC50 = 0.139 μM), and moderately inhibits PDGFR-β (IC50 of 0.236 μM) and c-Met (IC50 of 0.281 μM). VEGFR-2-IN-88 acts as a cell cycle inhibitor that arrests cells at the G0/G1 phase. VEGFR-2-IN-88 induces Apoptosis. VEGFR-2-IN-88 downregulates serum AST and ALT levels. VEGFR-2-IN-88 exerts selective anticancer effects. VEGFR-2-IN-88 reduces liver weight in in vivo models. VEGFR-2-IN-88 can be used in research related to hepatocellular carcinoma.
