Cyclic-di-GMP is a STING agonist and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
AV-105 is a Florbetapir (18F)-radiolabeled slyrylpyridine tosylate precursor extracted from patent WO2010078370A1, example 1.5. AV-105 can synthesize 18F-radiolabeled compounds, which are used for positron emission tomography (PET) imaging of neurodegenerative diseases of the brain[1].
Vitronectin (367-378) is a peptide corresponding to residues 367-378 of Vitronectin. Vitronectin is a multifunctional glycoprotein known in several human tumors for its adhesive role in processes such as cell growth, angiogenesis and metastasis[1].
Melanotan (MT)-II, a synthetic melanocortin receptor agonist, is an injectable peptide hormone used to promote tanning.
Fenspiride-d5 hydrochloride is the deuterium labeled Fenspiride hydrochloride. Fenspiride hydrochloride is an α adrenergic and H1 histamine receptor antagonist[1][2].
Tegileridine is the potent agonist of opioid receptor (MOR). Tegileridine is an oxa spiro derivative which reduces the side effects mediated by β-arrestin. Tegileridine has the potential for the research of pains and pains-related diseases (extracted from patent WO2017063509A1)[1].
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research[1][2].
N-(3-Oxooctanoyl)-DL-homoserine lacton is a member of N-Acyl homoserine lactone (AHL) from gram-negative bacteria, with stereochemistry-dependent growth regulatory activity for roots [1].
(1S)-1,4-Anhydro-1-C-(2,4-difluorophenyl)-D-ribitol is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Theodrenaline is a cardiac stimulant, also acts as an anti-hypotensive agent together with cafedrine.
Fosthiazate is a broad-spectrum nematicide against various plant parasitic nematodes, including Meloidogyne spp., Globodera spp., and Pratylenchus spp., through inhibiting the synthesis of acetylcholinesterase[1].
CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity[1].
20-Deoxyingenol is a natural compound.
Haloperidol D4' is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
NPC 200 is a potent and selective antagonist of Adenosine A1 Receptor. NPC 200 reverses NECA-induced left and right atrial depression with EC50s of 1.08 and 2.03 μM[1].
Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes[1][2].
Kaempferol-7,4'-dimethyl ether is found in Boesenbergia longiflora[1].
Sulfamonomethoxine-13C6 is the 13C6 labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
Lanreotide (BIM 23014) is a somatostatin analogue with antineoplastic activity. Lanreotide can be used for the research of carcinoid syndrome[1][2].
ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro[1][2].
NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8+ T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model[1].
TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation; enhances the degradation of both α-syn and tau, does not induce the degradation of GAPDH, enhances the degradation of intrinsically disordered proteins in cell culture; display a decrease in assembled 26S and an increase in 20S proteasome in treated cells.
S-Acetyl-PEG8-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
c-ABL-IN-1 is a novel selective c-Abl inhibitor that prevents neurodegeneration in parkinson’s disease.
N-Acetyl-S-(4-nitrophenyl)-L-cysteine is a cysteine derivative[1].
PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
Dichlorophenyl-ABA is an inhibitor of transthyretin (TTR) amyloid fibril formation, inhibiting aggregate formation in more than 80% in TTR L55P-expressing cells[1].