ap-4

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

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.

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

Broad spectrum EAA ligand

Group III mGlu receptor agonist

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

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].

1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 3.0 μM; it exhibits in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 56.3plusmn;0.4 and 46.0plusmn;0.3 M, respectively. It also inhibits LPS-induced NF-κB and AP-1 activations by interfering with the posttranslational modification (phosphorylation and or ubiquitinylation) of IRAK-1, disrupting TAK1-mediated activation of IKK and MAPKs signal transduction.

AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

AP-III-a4 hydrochloride (ENOblock hydrochloride) is a direct enolase (enolase) inhibitor with non-substrate analogs.AP-III-a4 hydrochloride inhibits metastasis of cancer cells in vivo and affects glucose homeostasis and can be used in bioassays.

GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP) when administered at doses of 25 and 50 mg kg. GYKI 52466 (30 mg kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.

PAR-4 Agonist Peptide, amide (AY-NH2), is an agonist of proteinase-activated receptor-4 (PAR-4).

NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that facilitates the nuclear import of cytosolic cargoes by utilizing the nuclear-localized bromodomain-containing protein 4 (BRD4) as a carrier for co-import and subsequent nuclear entrapment [1].

Linoleoyl Ethanolamide is an endocannabinoid agent. It acts by binding to TRPV1 increasing ERK phosphorylation and AP-1 dependent transcription in CB-receptor in an independent manner.

FOSL1 degrader 1 (4) is a potent T-5224-PROTAC that effectively degrades FOSL1 (AP-1), thereby suppressing the expression of cancer stemness genes in HNSCC. By degrading FOSL1, it inhibits tumor growth and effectively eliminates cancer stem cells in HNSCC tumors. This compound demonstrates an efficacy 30 to 100 times greater than that of T-5224.

PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)), is a selective activator of the proteinase-activated receptor-4 (PAR-4) that does not affect PAR-1 or PAR-2, and its activity can be inhibited by a PAR-4 antagonist.

ARP (Aldehyde reactive probe) is a chemical compound that serves as an aldehyde-reactive probe by specifically tagging AP sites in DNA with biotin residues. It is used to detect abasic sites, which are common forms of DNA damage and intermediates in mutagenesis and carcinogenesis. ARP is highly sensitive, capable of detecting abasic sites at the femtomolar level (fewer than 1 site per 10^4 nucleotides).