5'-O-DMTr-2'-O-methyl-N6-methyl adenosine 3'-CED phosphoramidite is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Fmoc-NH-PEG8-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Oxyclozanide is a salicylanilide anthelmintic drug that mainly acts by uncoupling oxidative phosphorylation in flukes.
Serelaxin (RLX-030), a recombinant form of human gene-2 relaxin targeting the RLN receptor, is a vasoactive peptide hormone with an antifibrotic activity[1][2][3].
Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties[1].
Xanthosine-5'-Triphosphate (5'-XTP), a nucleotide, is produced by deamination of purine bases[1].
Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3[1][2].
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: c-Metin vitro: MK-2461 inhibits the kinase activity of human c-Met with a mean IC50 of 2.5 nM in the presence of 50 μM ATP. Ron (IC50 = 7 nM) and Flt1 (IC50 = 10 nM) are inhibited by MK-2461 with similar potencies to c-Met (IC50 = 2.5 nM), whereas nine other kinases, including FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB, are found to be 8- to 30-fold less sensitive to MK-2461 than c-Met. [1]in vivo: MK-2461 inhibits c-Met signaling and tumor growth in tumor xenograft models in mice.[1]
Competence-Stimulating Peptide-12261, a sixteen peptide, is a fragment of competence-stimulating peptide. Competence-Stimulating Peptide, a quorum-sensing molecule, competence-stimulating peptide (CSP) which inhibits germ tube (GT) formation[1].
Pachypodol exerts antioxidant and cytoprotective effects in HepG2 cells[1].Pachypodol inhibits the growth of CaCo 2 colon cancer cell line in vitro(IC50 = 185.6 mM)[2].
2-Amino-3-chloropropanoic acid hydrochloride is an alanine derivative[1].
Gluten Exorphin A5 is a fragment from wheat gluten with neuroprotective effects. Gluten Exorphin A5 produces various effects not only in the peripheral nervous systems but also in the central nervous system[1].
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade[1][2][3].
Norbornene-NHS is a click chemistry reagent containing an azide group. Norbornene-NHS is a dienophile for conjugation via copper-free Click reaction with tetrazines[1].
Dimethylamiloride is a specific antiporter inhibitor[1].
CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM[1].
Influenza HA (307-319) is 13 amino acids 307 to 319 fragment of Influenza HA. Influenza HA is a glycoprotein found on the surface of influenza viruses[1].
SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (Mpro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19[1].
SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor with an IC50 of 1.3 μM. SIRT2-IN-10 can be used for the research of cancer and neurodegenerative disease[1].
A VHL ligand for PROTAC.
Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
2’-Deoxy-2’-fluoroinosine is a purine nucleoside analog. 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].
Boc-NH-PEG3-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1-Bromoheptane-d7 is the deuterium labeled 1-Bromoheptane[1].
Mal-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Dermaseptin-B3 inhibits the growth of Gram-positive and Gram-negative bacteria (MIC: 1.3, 2.3, 5.0, 2.6, 2.3 μM for S. aureus, P. aeruginosa, P. aeruginosa, E. (ATCC 25922), E. (54127) respectively). Dermaseptin-B3 also inhibits tumor cell proliferation[1][2].
Gomisin S is a dibenzocyclooctadiene lignan[1].
(S)-2-amino-3,3-dimethylbutanoic acid is a leucine derivative[1].
PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound PAC1. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).