Trk Receptor Inhibitor

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.

TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC₅₀ of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity.

c-Fms-IN-3 is an orally active c-Fms (CSF1R) kinase inhibitor (IC₅₀ = 0. 8 nM). c-Fms-IN-3 inhibits CSF1R kinase activity and reduces macrophage populations. c-Fms-IN-3 reduces bone erosion, pannus invasion, cartilage damage, and inflammation in collagen (HY-NP003)-induced arthritis mouse model. c-Fms-IN-3 is useful for arthritis research.

MNAC13 is a kind of mouse IgG1 chimeric antibody, targeting to human TrkA. MNAC13 inhibits the NGF dependent signaling pathway by specifically binding to TrkA receptors. MNAC13 has good analgesic effect and long-lasting efficacy. MNAC13 can be used for researches on inflammatory and chronic pain.

Povovetug is a humanized IgG1κ chimeric monoclonal antibody inhibitor targeting NGF/bNGF. Povovetug has a significant analgesic activity. Povovetug can be used for central neuroinflammation like chronic radicular pain research.

Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers.

Luvagrobart is an anti-NGF human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC₅₀=2.6 nM). CZS-241 inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 (PLK4) (IC₅₀=2.6 nM). CZS-241 hydrochloride inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 hydrochloride induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 hydrochloride shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF (IC₅₀: 21 nM for human TrkA in PathHunter assay). TrkA/NGF-IN-1 shows an analgesic effect in a rat incisional pain model.

Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC₅₀ values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.

1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors.

Anti-MUSK Antibody is a humanized antibody expressed in CHO that targets MUSK. The Anti-MUSK Antibody contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 143.86 kDa. For the isotype control of Anti-MUSK Antibody, please refer to Human IgG1 (L234A/L235A) kappa, Isotype Control (HY-P991207).

Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC₅₀ values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.

Anti-NGF/bNGF Antibody is a CHO-expressed humanized antibody that targets NGF/bNGF. Anti-NGF/bNGF Antibody has a huIgG2 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 144.14 kDa. The isotype control for Anti-NGF/bNGF Antibody can be referenced as Human IgG2 kappa, Isotype Control (HY-P99002).

Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC₅₀s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC₅₀s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkA^G595R and TrkA^G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC₅₀=182 nM). LPM4870108 exhibits anti-tumor activity.

FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC₅₀s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML).

PF-06733804 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC₅₀ value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.