pdgf 2

Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K，是抗寄生虫，抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂，也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。

AG-494 (Tyrphostin B48) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂，IC50为0.7 μM。它阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。它抑制 EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化，IC50为 1.1、39、45 和 6 μM。

JNJ-10198409 是相对选择性的、ATP 竞争性的、具有口服活性的血小板衍生生长因子受体酪氨酸激酶抑制剂，其IC50=2 nM。它对PDGFR-β激酶 (IC50=4.2 nM) 和PDGFR-α激酶 (IC50=45 nM) 有较好的抑制作用。它是双重机制的抗血管生成和肿瘤细胞的抗增殖剂。

WQ-C-401 是一种抗PDGFR的口服抑制剂，其作用机制是通过浓度依赖性抑制PDGFR自身的磷酸化，从而抑制细胞增殖。该化合物对PDGFRαY849和PDGFRβY1021的磷酸化具有较强的抑制效果，EC50值分别为3.5和5.8 nM。此外，WQ-C-401能够抑制PDGF-BB引起的ERK1 2磷酸化，有效阻止PASMCs的增殖和迁移，减少胶原 I 的合成并提升α-SMA的表达，有助于防止肺血管重塑。该化合物在肺动脉高压研究领域显示出潜在应用价值。

2-Methyl-3-phenylquinoxaline (compound 38) 作为一种有效的血小板衍生生长因子受体酪氨酸激酶 (PDGF-RTK) 抑制剂，对完整细胞中的PDGFR激酶显示出抑制活性，其半抑制浓度 (IC50) 超过 100 μM。

Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties.1,2 It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM).1 Quazinone (10-300 μg kg) increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner, as well as decreases systolic and diastolic blood pressure.2 It also inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smooth muscle cells in a concentration-dependent manner.3

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).

The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formationin vivo[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injuryin vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg kg day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation[3].

Corynoxeine 是从钩藤中分离的一种天然产物，是 PDGF-BB 诱导血管平滑肌细胞 (VSMCs) 增殖过程中的 ERK1 ERK2抑制剂。

FGF PDGF VEGF RTK Inhibitor is a potent, reversible, atp-competitive inhibitor against pdgfrβ, fgfr-1, and vegfr-2 (ic50 = 20, 90, and 240 nm, respectively) and effectively suppresses vegf-stimulated proliferation of hmvecs (ec50 = 420 nm).

Methylnissolin 是从黄芪中分离的一种天然产物，可抑制血小板衍生生长因子 (PDGF)-BB 诱导的细胞增殖，IC50为 10 μM。。它通过抑制ERK1 2MAP 激酶级联反应抑制 PDGF-BB 诱导的血管平滑肌细胞增殖。它还抑制 PDGF-BB 诱导的细胞外信号调节激酶 1 2 (ERIC1 2) 丝裂原活化蛋白 (MAP) 激酶的磷酸化，具有抗菌和抗癌作用。