ap-4

AP-4 is an antagonist of the NMDA glutamate receptor.

L-APB is an effective and specific agonist for the group III mGluRs (EC50s: 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively).

broad spectrum excitatory amino acid receptor antagonist

Group III mGlu receptor agonist

L-AP4 (L-APB) monohydrate is a potent and specific agonist for group III mGluRs, with EC50s of 0.13, 0.29, 1.0, and 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively [1][2].

MSOP is a selective antagonist of group III metabotropic glutamate receptor (KD of 51 μM for the L-AP4-sensitive presynaptic mGluR).

DL-AP4, also known as 2-Amino-4-phosphonobutyric acid, is a competitive glutamate antagonist with defined binding affinity that is widely used to selectively inhibit glutamatergic neurotransmission, making it an essential experimental compound for probing synaptic signaling mechanisms and functional circuitry in central nervous system and visual system research.

AP-4-139B is a potent inhibitor of Heat Shock Protein 70 (HSP70), with an IC50 value of 180 nM. HSP70 is a protein that is overexpressed in various cancers and plays a critical role in the survival and proliferation of tumor cells. AP-4-139B demonstrates significant cytotoxicity in tumor cells, particularly in colorectal cancer cells, making it useful for cancer research.

TAK1/MAP4K2 inhibitor 1 (compound 5) is a dual kinase inhibitor of TAK1 and MAP4K2 with IC50 values of 41.1 nM and 18.2 nM, respectively.

GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA).

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Broad spectrum EAA ligand

GNE-220 is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.

KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

MAP4K4-IN-3 (Compound 17), a serine/threonine protein kinase, may be a viable target for antidiabetic agents.

MAP4K4-IN-6 (Compound 15f) is a MAP4K4 inhibitor with an IC50 of 80 nM. It reduces the phosphorylation of c-Jun and exhibits neuroprotective effects. Additionally, MAP4K4-IN-6 enhances the vitality of motor neurons and can be utilized in the study of amyotrophic lateral sclerosis (ALS).

HPK1-IN-52 is an effective orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor, displaying anti-tumor activity with an IC50 value of 10.4 nM.

Ap4dT serves as an inhibitor of human adenylate kinase isozyme 1 (hAK1), effectively suppressing the synthesis of ATP and ADP, with IC50 values of 42 μM and 38 μM, respectively.

HPK1-IN-56 (Compound A29) is an HPK1 inhibitor with an IC50 of 2.70 nM. It inhibits downstream p-SLP76 in Jurkat T cells with an IC50 of 8.1 nM. Additionally, HPK1-IN-56 induces IL-2 production in human PBMCs. This compound exhibits anticancer properties, enhancing T cell cytotoxicity and the antitumor efficacy of anti-PD-1 antibodies.

AAP4 is a potent inhibitor of OfChi-h and OfHex1, exhibiting Ki values of 29.3 nM and 4.9 μM, respectively. It also demonstrates insecticidal activity against the lepidopteran pest Ostrinia furnacalis.

TFAP4/Wnt/β-catenin-IN-1 (Compound A61) is an orally active inhibitor targeting the TFAP4/Wnt/β-catenin pathway. Known for its potent anticancer properties, it effectively targets various cancer cells, including those of gastric, lung, and breast cancer, with the strongest activity observed in MGC-803 gastric cancer cells (IC50: 3.92 μM). By inhibiting the TFAP4/Wnt/β-catenin signaling pathway, it induces apoptosis and S phase cell cycle arrest. TFAP4/Wnt/β-catenin-IN-1 is applicable for gastric cancer research.

metabotropic glutamate receptor modulator

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.

Ap44mSe is a potent and selective antitumor agent. Ap44mSe effectively depletes cellular Fe, resulting in transferrin receptor-1 up-regulation, ferritin down-regulation, and increased expression of the potent metastasis suppressor, N-myc downstream regula