Muscarine ((+)-Muscarine) chloride is a toxin that can stimulate the parasympathetic nervous system. Muscarine is a prototype muscarinic acetylcholine receptor agonist[1][2].
Tos-PEG2-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1-Bromo-4-fluorobenzene-d4 is the deuterium labeled 1-Bromo-4-fluorobenzene[1].
Uridine 13C-3 is the 13C labeled Uridine[1].
Mesoxalate (Ketomalonic acid) a dicarboxylic acid and a ketonic acid which blocks HIV-1 reverse transcriptase (RT), with the IC50 of 2.2 μM[1][2].
PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation[1].
TG693 is an orally active inhibitor of CLK1. TG693 regulates the mutated exon 31 of the dystrophin gene in vivo. TG693 is used in Duchenne muscular dystrophy (DMD) research[1].
Modotuximab (Anti-Human EGFR Recombinant Antibody) is an IgG1κ-type chimeric antibody targeting human EGFR protein. Modotuximab contains a portion of Futuximab that binds to two independent, non-overlapping epitopes on EGFR. Modotuximab promotes cross-linking of EGFR on the cell surface and promotes EGFR cellular internalization and degradation. Modotuximab has antitumor activity in vivo[1].
USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM[1].
N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines[1].
Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
Tanshinlactone is a seco-abietanoid that can be isolated from Salvia miltiorrhiza. Tanshinlactone is a coronavirus (CoV) inhibitor. Tanshinlactone modulates interleukin-2 and interferon-γ gene expression[1][2].
LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract[1].
RSV/IAV-IN-2 (compound 14c) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-2 has lesser cytotoxicity than the clinical drug, Ribavirin. RSV/IAV-IN-2 has the potential for the research of RSV and/or IAV infections[1].
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice[1][2][3].
(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) is a somatostatin analog with Kds of 0.61, 11.05, 23.5, 1200 and >1000 nM for SSTR5, SSTR3, SSTR2, SSTR1 and SSTR4, respectively[1].
Isoescin Ie is a derivative of Aescine in Aesculi Semen extract[1].
5-PT is a serotonin derivative that can be functionalized with various reporter groups via click chemistry to investigate protein serotonylation. 5-PT can be used in vivo to observe endogenous protein serotonylation[1].
Antibacterial agent 98 (compound g37) is a potent and orally active antibacterial agent. Antibacterial agent 98 inhibits the ATPase activity of Gyrase B and impairs Staphylococcus aureus (S. aureus ) DNA supercoiling. Antibacterial agent 98 shows antibacterial activity and not induce resistance development of MRSA (methicillin-resistant S. aureus)[1].
kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.
Sorafenib (Bay 43-9006) is a potent multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM; weakly inhibits L-selectin (IC50=2.9 uM) and >10 uM for P-selectin; not only mobilizes AML cells out of protective niches but also blocks NF-kB activation and prevents this E-selectin-mediated chemoresistance, thereby enhancing the therapeutic effects of standard chemotherapy; also overcomes MM metastasis and chemoresistance. Blood Cancer Phase 2 Clinical
Proflavine (3,6-Diaminoacridine) dihydrochloride, an acridine dye, is a DNA intercalating agent and Anti-microbial agent. Proflavine dihydrochloride behaves as a pore blocker for Kir3.2. Proflavine dihydrochloride is a potential lead compound for Kir3.2-associated neurological diseases[1][2][3].
Isoamylase (Glycogen α-1,6-glucanohydrolase) catalyzes the hydrolysis of α-1,6-glycosidic linkages in glycogen, amylopectin and α/β-limit dextrins[1].
Mitiglinide calcium hydrate is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. IC50 value:Target: KATP channel
Tideglusib is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3βWT (1 h preincubation) and GSK-3βC199A (1 h preincubation), respectively.
Cbz-NH-PEG8-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.
(+)-Syringaresinol, a lignan, is a NFAT transcription factor inhibitor, with an IC50 of 329.4 μM. (+)-Syringaresinol also can be used for the research of lymphocytic leukemia[1][2].
Wighteone is a compound isolated from the aerial parts of Genista ephedroides[1].