Trk Receptor Inhibitor

TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC₅₀ values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA^G595R, TRKA^F589L, and TRKA^G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells.

TRK-IN-16 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-16 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-21).

TRK-IN-26 (compound 12) is a TRK inhibitor with potential for cancer research.

GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC₅₀ values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD⁺ levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research.

GZ-389988 is a potent pan-TRK inhibitor with IC₅₀ values ​​of 0.3, 0.1, and 0.5 nM for TRKA, TRKB, and TRKC, respectively. GZ-389988 can be used to study NTRK fusion-positive tumors.

RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC₅₀=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI₅₀ of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase.

TrkB-IN-2 is a TrkB inhibitor. TrkB-IN-2 exhibits anticancer activity against neuroblastoma. TrkB-IN-2 can be used for research on neuroblastoma.

(3S,4R)-PF-6683324 is a tropomyosin-related kinase (Trk) inhibitor extracted from patent WO2015092610A1 example 9. (3S,4R)-PF-6683324 has the potential for the research of pain and cancer.

TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC₅₀s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA^G595R, TRKA^G667C, TRKA^F589L, TRKC^G623R, TRKC^G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model.

Licorisoflavan A (7-O-Methyllicorisoflavan B) is a isoflavan-quinone, that can be isolated from Glycyrrhiza uralensis. Licorisoflavan A exhibits anti-inflammatory and antimicrobial properties. It can inhibit the secretion of IL-6 and chemokines by LPS-stimulated macrophages in a concentration-dependent manner, and also suppress the secretion of MMP-7, MMP-8, and MMP-9 in macrophages. Licorisoflavan A exertes potent antidepressant-like effects involving BDNF-TrkB pathway and AMPA receptors.

TRK-IN-14 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-14 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-47).

Cyclotraxin B TFA is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B TFA inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC₅₀ of 0.30 nM. Cyclotraxin B TFA has analgesic and anxiolytic effects.

Protein kinase inhibitor 5 sulfate hydrate is a potent TRK-A inhibitor with an IC₅₀ value of 1.8 nM. Protein kinase inhibitor 5 sulfate hydrate inhibits cell viability.

Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC₅₀=3.0 nM and 104 nM respectively).

Trk-IN-2 is an orally active pan-Trk kinase inhibitor with an TrkA IC₅₀ of 9 nM. Trk-IN-2 exhibits pharmacodynamic effects in rat models of inflammatory pain and neuropathic pain.Trk-IN-2 can be used for the research of inflammatory pain, neuropathic pain.

hTrkA-IN-2 is a selective hTrkA allosteric inhibitor with an IC₅₀ value of 3.9 nM.

Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC₅₀ values of 0.55 nM, 25.1 nM and 5.4 nM against TRK^WT, TRK^G595R and TRK^G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC₅₀ values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA^WT, Ba/F3-ETV6-TRKB^WT, Ba/F3-LMNA-TRK^G595R and Ba/F3-LMNA-TRKA^G667C, respectively.

PF-07245303 is a ITK/TRK inhibitor. PF-07245303 reduces the production of inflammatory cytokines such as IL-4 and IFNγ, and inhibits the phosphorylation of PLCγ1. PF-07245303 inhibits nerve growth factor-induced basophil activation and the phosphorylation of TRKA. PF-07245303 reduces oxazolone-induced ear swelling in mouse ear tissues. PF-07245303 is applicable to research related to atopic dermatitis.

Protein kinase inhibitor 5 is a potent TRK-A inhibitor with an IC₅₀ value of 1.8 nM. Protein kinase inhibitor 5 inhibits cell viability.