PTP1B-IN-8 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1[1].
GSK3036656 (GSK070) is a potent, selective and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase, with an IC50 of 0.20 μM. GSK3036656 can be used for the research of tuberculosis[1].
Tuberculosis inhibitor 7 (compound 2d) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of 0.63 μM) and Mycobacterium marinum (MIC90 of 0.63 μM)[1].
FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459). FC-11 degrades FAK in various cells, with DC50s of 310 pM in TM3, 80 pM in PA1, 330 pM in MDA-MB-436, 370 pM in LNCaP, and 40 pM in Ramos cells[1].
N2-Isobutyryl-2'-O-methylguanosine (N2-IBU-2'-OME-RG) 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].
Kievitone, an isoflavanone, could be isolated from hypocotyls of Phaseolus vulgaris L. infected with Rhizoctonia solani Kühn. Kievitone has antifungal activity and antitumor activity[1][2].
Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10[1].
Tofacitinib is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM.
3,5-Dimethoxyphenol is a toxin metabolite, found in human consuming yew leaves[1].
Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory drug). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research[1].
GNE-781 is a highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nΜ, respectively.
Azide-C2-SS-C2-biotin is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Fulimetibant is a bradykinin receptor antagonist[1].
Delphinidin 3,5-diglucoside is an anthocyanin, and can be isolated from Punica granatum[1].
L-2-Aminooxy-3-phenylpropanoic acid hydrobromide is a potent inhibitor of L-phenylalanine ammonia-lyase[1].
Lynamicin B is a potential pesticide by acting as a lepidoptera-exclusive chitinase inhibitor with a Ki value of 8.76 μM.
MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK-1 potently activated phagocytic leukocytes and could enhance Pertussis Toxin (HY-112779)-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity[1][2][3][4].
Pamidronate disodium pentahydrate is a nitrogen-containing bisphosphonate, used to prevent osteoporosis.
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs)[1][2].
GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
Morin 3-O-β-D-glucopyranoside is a natural flavonoid with antifungal, anticancer and antioxidant activities. Morin 3-O-β-D-glucopyranoside inhibits reverse transcriptase, protein-tyrosine kinase and xanthine oxidase, and also shows anti-HIV, antiarteriosclerotic, and superoxide scavenging activities[1].
Hexaethylene glycol phosphoramidite (Spacer Phosphoramidite 18) is an amidite reagent for oligonucleotide synthesis. Hexaethylene glycol phosphoramidite can be used as a linker in synthesis of nucleotide chain and qPCR probes[1][2].
Pyrocatechol monoglucoside is a phenolic glycoside that can be isolated from Itoa orientalis[1].
Trimebutine-d5 is the deuterium labeled Trimebutine. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects[1][2].
TM5441 is a plasminogen activator inhibitor-1 (PAI-1); inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM.
Tolmetin sodium is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin sodium is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
μ-Conotoxin GIIIB is a 22-residue polypeptide that can be isolated from the venom of piscivorous cone snail Conus geographus. μ-Conotoxin GIIIB is a NaV1.4 channel inhibitor. μ-Conotoxin GIIIB blocks muscle cell's contraction[1][2][3].
1,2-Dihydrotanshinone (1,2-Dihydrotanshinquinone) is an abietane diterpene. 1,2-Dihydrotanshinone inhibits the formation of the pathogenic complex formed between (CUG)n-RNA and the splicing-factor muscleblind-like 1 (MBNL1). 1,2-Dihydrotanshinone can be used for the research of myotonic dystrophy type 1[1][2].
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines[1].