JNJ-67569762 is a selective BACE1 inhibitor targeting the S3 pocket (IC50 = 2.7 nM).
STING-IN-6 (compound 50) is a potent STING inhibitor with a pIC50 of 8.9. STING-IN-6 has the potential for immunity research[1].
5'-Deoxy-5'-iodouridine 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].
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect[1].
5-Fluoro-2′-deoxy-UTP can be used as a substrate for DNA synthesis[1].
N-Methyl-N'-methyl-O-(m-PEG4)-O'-(azide-PEG4)-Cy3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AZD1390 is an ATM inhibitor.
WAY-655978 is an active molecule.
(S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein[1].
3-Feruloyl-4-caffeoylquinic acidis acaffeoyl, feruloyl quinic acidderivativeisolated fromroasted C.arabica[1].
Staphyloferrin A is a siderophore protein that can be combined with antibiotics to study drug-resistant bacteria that cause skin diseases[1].
Luteolin 7-diglucuronide is the major flavonoid isolated from Aloysia triphylla and Verbena officinalis[1].
VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity[1].
13-Epijhanol (compound 5) is a diterpenoid compound isolated from Grindelia scorzonerifolia[1].
SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1)[1].
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice[1].
A-425619, a potent and selective TRPV1 receptor antagonist, is effective in alleviating acute and chronic inflammatory pain and postoperative pain[1].
Thiol-PEG12-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
rac-Rotigotine Hcl is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM. IC50 Value: 0.69 nM(Ki)Target: D-2 receptorin vitro: rac-Rotigotine showed high potency (Ki = 0.69 nM) and selectivity for D-2 receptors as compared to its potency and selectivity at various other neuronal receptors (Ki in nM): D-1 (678) dopamine, alpha 1-(534) and alpha 2-(195) adrenoceptor, S1-(6940) and S2-(5900) serotonin and muscarine (2660). Very low activity (Ki greater than 10(-5) M) was seen at the beta-adrenoceptor, A1-adenosine, GABAA and benzodiazepine receptors. Furthermore, rac-Rotigotine inhibited the calcium-dependent release of [3H]dopamine (IC50: 4 nM) and [3H]acetylcholine (IC50: 6.3 nM) from rabbit striatal slices in the nanomolar range. These effects of rac-Rotigotine were mediated through activation of D-2 dopamine autoreceptors and D-2 dopamine heteroreceptors, respectively.in vivo: Presynaptic dopaminergic activity in vivo was measurable as an inhibition of the locomotor activity of mice, and in this model rac-Rotigotine was more effective than apomorphine. Moreover, the effect of rac-Rotigotine could be antagonized by sulpiride but not by yohimbine. rac-Rotigotine was equipotent with apomorphine in inducing circling behaviour in 6-OHDA-lesioned rats. rac-Rotigotine had almost no serotonergic activity in vivo.
Malvidin (chloride) is a bioactive compound isolated from Oryza sativacv. Heugjinjubyeo. Malvidin shows cytotoxicity through the arrest of the G2/M phase of cell cycle and induction of apoptosis. Malvidin can be used for the research of cancer[1].
MS-PEG3-dodecyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(E)-1α,25-Dihydroxyprevitamin D3 is a structurally related analog of 1α,25(OH)2D3[1].
COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB[1].
KKEDVV-Abu-CS-Abu-SYKK-NH2 is a peptide. KKEDVV-Abu-CS-Abu-SYKK-NH2 can be used for various biochemical research.
ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC50 of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer[1].
Ligustrosidic acid is a natural compound isolated from ligustrum japonicum and ligustrum lucidum[1].
Phenaglycodol belongs to the group of butanediolsa with anxiolytic and anticonvulsant porperties. Phenaglycodol has orally bioactivity[1].
DBCO-PEG4-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-amine can be used in the synthesis of FPM-PEG4-DBCO (a homobifunctional azide-to-azide cross-linker)[1].
SERCA2a activator A is a novel sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a (SERCA2a) activator that activates the Ca2+-dependent ATPase activity of cardiac SR vesicles but not that of skeletal muscle SR vesicles that lack of phospholamban (PLN); binds to PLN (Kd=75 uM), attenuates its inhibition of SERCA2a; enhances systolic and diastolic functions in rat hearts.
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models[1].