Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal.
MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). Has potential to treat tumor-induced bone disease (TIBD).
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ?glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT.
Heterocyclyl carbamate derivative 1 is a heterocyclyl carbamate derivative that may be used for the research of inflammatory and neurological diseases.
Deacetylanisomycin is a potent growth regulator in plants and an inactive derivative of Anisomycin. Anisomycin is a potent protein synthesis inhibitor.
DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.
CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.
Eperisone is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. Eperisone is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect.
TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.
hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor
SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM.
DPA-714 is a selective ligand for the translocator protein (TSPO) currently under evaluation for several clinical applications.It is also a PET tracer binding the TSPO receptor and highly expressed in myeloid cells.
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity.
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats.
