Trk Receptor Inhibitor

PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC₅₀ values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain.

Fasinumab (Anti-Human NGF) is a human IgG4 monoclonal antibody to nerve growth factor (NGF). Fasinumab can be used in acute sciatica and knee osteoarthritis (OA) studies.

TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC₅₀ of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain.

Cannflavin B is a flavonoid compound that can be isolated from Cannabis sativa L. Cannflavin B is inhibitors of PGE₂ release (IC₅₀: 0.7 μM), mPGES-1 (IC₅₀: 3.7 μM), and 5-lipoxygenase. Cannflavin B has multiple activities such as anti-inflammatory, antioxidant, anti-glycation, anti-ferroptosis, anti-tumor, and anti-Leishmania (IC₅₀: 14 μM). Cannflavin B can also inhibit the TrkB-BDNF signaling pathway.

DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a K_i value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research.

Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC₅₀ = 0.81 nM; TRKB IC₅₀ = 0.145 nM; TRKC IC₅₀ = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma.

Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC₅₀ of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases.

Fulranumab is a human IgG2 monoclonal antibody against nerve growth factor (NGF) and can be used for the research of pain.

TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC₅₀=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects.

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.

PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

2-Bromo-6-methoxynaphthalene is an active intermediate in the production of anti-inflammatory agents like Naproxen and Nabumetone by Heck reaction. 2-Bromo-6-methoxynaphthalene has potential anti-inflammatory properties and Tyrosine-protein inhibitor properties. 2-Bromo-6-methoxynaphthalene can be used for the research of cancer.

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC₅₀ of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC₅₀s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

Pz-1 is a potent RET and VEGFR2 inhibitor with IC₅₀s of less than 1 nM for both wild type kinases.

ALK-IN-28 (compound 22) is an inhibitor of anaplastic lymphoma kinase (ALK).

CH7057288 is a potent and selective TRK inhibitor. CH7057288 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC₅₀s of 4.7 and 1 nM.

Ganglioside GM1-binding peptide p3 is a synthetic peptide that can specifically bind to the pentasaccharide part of GM1 ganglioside. The dynamic transformation of Ganglioside GM1-binding peptide p3 may play an important role in the function of GM1 as a multiple receptor, such as in the classical pathway of cholera toxin infection. Ganglioside GM1-binding peptide p3 can be used to study the interaction between GM1 and its ligands.