TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively.
Ammelide-13C3 is the 13C3 labeled Ammelide.
Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating Nrf2 signaling pathway.
2-nonyl-3-hydroxy-4-Quinolone (C9-PQS) is a quinolone compound produced by P. aeruginosa and other related bacterias. 2-nonyl-3-hydroxy-4-Quinolone is a quorum sensing (QS) signal molecule that controls the expression of many virulence genes as a function of cell population density[1].
L-Asparaginase (L-ASNase), a hydrolase that catalyzes the conversion of L-asparagine, used in acute lymphoblastic leukemia treatment. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis[1].
tert-Butylamine-d9 Hydrobromide is the deuterium labeled tert-Butylamine Hydrobromide[1].
Lib2-1, a macrocyclic peptide, is an IL-17C/IL-17RE interaction inhibitor. Lib2-1 can be used for autoimmune and inflammatory diseases research[1].
Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease.Target: mAChRBenzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics. Symptoms of Parkinson's disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor [1, 2].Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). BZT analogues also exhibit varied binding affinities for muscarinic M(1) and histamine H(1) receptors. The BZT analogues showed a wide range of histamine H(1) receptor (K(i)=16-37,600 nM) and DAT (K(i)=8.5-6370 nM) binding affinities [3].
8-Allylthioadenosine 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].
SCH 23390 hydrochloride is a potent dopamine receptor D1 antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5.
2'-Deoxy-8-methylthioguanosine 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].
DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
ODIPY Green 8-P2M is a novel thiol-reactive fluorescence probe based on the BODIPY fluorophore, the fluorescence is strongly quenched by d-PeT and then can be restored after reaction with thiol, resulting in an extremely high signal-to-noise ratio. ODIPY Green 8-P2M can be useful for detecting extremely low concentrations of protein in the gel after SDS-PAGE[1].
DMT-2'-F-Bz-dC is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester prodrug of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice[1].
Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity[1].
1,2-Hexadecanediol is a reducing agent. 1,2-Hexadecanediol facilitates the decomposition of the metal-organic precursor, forms an intermediate Co2+Fe3+-oleate complex[1].
Bezeparsen is a PCSK9 synthesis inhibitor[1].
5-(Hydroxymethyl)-2′,3′-O-(1-methylethylidene)uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Cyclo(-Leu-Phe) is a cyclic peptide composed of leucine and phenylalanine, forming a ring structure through peptide bonds[1].
EPZ031686 is an orally available SMYD3 inhibitor with an IC50 of 3 nM in cell-free assay.
Brevianamide Q (Compound 3) is an alkaloid derived from Aspergillus versicolor[1].
Substance P (alligator), a Substance P (Substance P (HY-P0201)) extracted from alligator, is a neuropeptide. The primary structure of Substance P (alligator) is: Arg-Pro-Arg-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2[1].
Petunidin-3-O-(6-O-p-coumaryl)-5-O-diglucoside is a natural product that can be isolated from grapes[1].
Triethylene glycol monododecyl ether is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ajugasterone C is an ecdysteroid isolated from Leuzea carthamoides. Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to Carrageenan-induced inflammation in Sprague Dawley rats[1][2].
Eprodisate is a new compound designed to interfere with interactions between amyloidogenic proteins and glycosaminoglycans and thereby inhibit polymerization of amyloid fibrils and deposition of the fibrils in tissues[1]. Eprodisate slow the progression of AA amyloidosis-related renal disease and has possible applicability to other types of amyloidosis[2].
N-(Boc-PEG1)-N-bis(PEG2-propargyl) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC50 values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity[1].
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research[1].