PDGFRβ Inhibitor

Rinucumab (REGN 2176) is an anti-PDGFR-β antibody. Rinucumab is used for research on neovascular age-related macular degeneration.

Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.

Ilorasertib (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).

NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC₅₀s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.

Flumatinib (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.

N-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.

Hypothemycin, a fungal polyketide, is a multikinase inhibitor with K_is of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.

(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC₅₀s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

GZD856 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-Abl^T315I 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.

Myricanol 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.

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC₅₀s of 8, 4, 7 and 9 nM in cell assay, respectively.

Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC₅₀s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.

WQ-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.

PD-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.

GW296115 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.

KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.

Sunitinib (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.

BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC₅₀ value of 23 nM and K_i value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC₅₀ values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research.

Sunitinib-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.

AC710 is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.