(R)-RP-6306 (183) can be used for the research of Myt1 mediated diseases and kinds of cancer for slowing the progression of cancer[1].
Cefmenoxime (SCE-1365) is a new semisynthetic cephalosporin antibiotic. Cefmenoxime has antibacterial activity against a wide variety of gram-positive and gram-negative bacteria[1][2].
Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.
Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM[1]. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome[1].
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1][2].
JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor, with IC50 values of 38 and 600 nM for JAK3 and JAK2, respectively. JAK3-IN-14 shows inhibitory of IL-4 and IL-3 induced TF-1 cell proliferation, with IC50 values of 600 and 500 nM, respectively[1].
Methylamino-PEG1-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Metallo-β-lactamase-IN-5 (compound 5c) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-5 shows inhibitory activity against MBLs NDM-1 and VIM-1. Metallo-β-lactamase-IN-5 inhibits HUVECs with an IC50 of 45 μg/mL. Metallo-β-lactamase-IN-5 plus Imipenem exhibits synergistic antimicrobial activity[1].
Izuralimab is a bispecific IgG1 antibody targeting inducible T-cell costimulator (ICOS/CD278) and PD-1[1].
DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB)[1].
D,L-3-Indolylglycine is an unnatural amino acid that is very similar to Tryptophan, with the indole moiety directly attached to the α-position. Target:D,L-3-Indolylglycine may be useful in the design of functional proteins. A study describes the inclusion of a similar aza-indoylglycine moiety in petidomimetics with the purpose of functionally replacing tryptophan moieties.
TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
Arjungenin, a triterpene isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor[1][2].
(Z)-2-Angeloyloxymethyl-2-butenoic is a natural product that can be found in the roots of Anthriscus sylvestris Hoffm.[1]
Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL)[1].
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity[1].
Ceftobiprole medocaril is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA).
DBCO-PEG9-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Fmoc-D-Tyr(tBu)-OH is a tyrosine derivative[1].
Acrylodan, reacted with thiols, is sensitive to the local environmental dipolarity and dynamics within the binding pocket surrounding Cys34[1][2].
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer[1][2][3].
Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells[1].
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5[1].
Benidipine hydrochloride is a dihydropyridine calcium channel blocker for the treatment of high blood pressure (hypertension).
Nardosinone, isolated from Nardostachys chinensis, is the first enhancer of the neuritogenic action of dbcAMP and staurosporine. Nardosinone may become a useful pharmacological tool for studying the mechanism of action of not only nerve growth factor (NGF) but also both the neuritogenic substances[1].
2-Nitrophenyl α-D-galactopyranoside, a nitrophenyl derivative, is a substrate to test for hydrolytic activity of glycosyl hydrolase[1].
3-(1-Cyanoethyl)benzoic acid (DF2107Y) is a benzoic acid that can be used to screen cobalt containing nitrile hydratases (NHases)[1].
Cap-dependent endonuclease-IN-25 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-25 is a macrocyclic pyridotriazine derivative. Cap-dependent endonuclease-IN-25 has the potential for the research of viral infections caused by viruses belonging to the Orthomyxoviridae family (extracted from patent WO2020075080A1, compound 4)[1].
Demethoxydeacetoxypseudolaric acid B is a metabolite of the glucoside of pseudolaric acid C2 (PC2)[1].
N-(2,3-Dihydro-1,4-benzodioxin-6-ylsulfonyl)-beta-alanine is an alanine derivative[1].