pdgf-1

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) 是咖啡酸的苯乙醇酯，是蜂巢蜂胶的生物活性成分。它抑制核转录因子 NF-kappa B 的激活，具有抗肿瘤、细胞保护和免疫调节活性。它抑制 PDGF 诱导的血管平滑肌细胞增殖。

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) (PDGF Receptor Tyrosine Kinase Inhibitor III)是一种多激酶抑制剂，可抑制 PDGFR、EGFR、FGFR、PKA 和 PKC 等。PDGFR Tyrosine Kinase Inhibitor III 可用于肌萎缩侧索硬化症的研究。

PD-161570 是一种有效的 ATP 竞争性人 FGF-1 受体抑制剂，IC50 为 39.9 nM，Ki 为 42 nM。它还是骨形态发生蛋白 (BMPs) 和TGF-β信号抑制剂。它抑制PDGF 刺激的自磷酸化和FGF-1受体磷酸化，IC50分别为 450 和 622 nM。它抑制 PDGFR、EGFR 和 c-Src 酪氨酸激酶，IC50 值分别为 310、240 和 44 nM。

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。

Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) 是多激酶抑制剂。它有用于导致与酪氨酸激酶活性异常或失控有关的疾病或失调的潜力，特别是与c-Kit，PDGF-R，Bcr-abl 活性相关的疾病。

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。

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

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].

Physalin B 是茄科植物的主要活性化合物之一，具有广泛的生物活性，可用于治疗炎症湿疹和疱疹等疾病。Physalin B 通过激活 PI3K Akt 通路抑制 NF-κB 和 NLRP3，从而改善脂多糖诱导的急性肺损伤造成的炎症反应。Physalin B 通过激活 Nrf2 通路抑制 PDGF-BB 诱导的 VSMC 增殖、迁移和表型转化。Physalin B 通过抑制 LAP2α-HDAC1 介导的胶质瘤相关癌基因 1 的去乙酰化和肝星状细胞活化来发挥抗肿瘤活性。

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).