Rivanicline oxalate (RJR-2403 oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).
Porgaviximab is a monoclonal antibody that can be used Ebola infection research[1].
MRS2298? is a potent acyclic P2Y1 receptor antagonist with a Ki of 29.6 nM. MRS2298 inhibits the ADP-induced aggregation of human platelets with an IC50 of 62.8 nM. MRS2298 inhibits Ca2+ rise in platelets with an IC50 of 810 nM[1].
Longdaysin is a CK1α, CK1δ, and extracellular signal-regulated kinase 2 (ERK2) inhibitor with IC50s of 5.6 µM, 8.8 µM, and 52 µM, respectively[1][2].
F-PEG2-COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Lucenin 3 is a bioactive flavonoid[1].
L-Biotin-NH-5MP-Br is a biotin-conjugated 5-Methylene pyrrolone (5MP). 5-Methylene pyrrolones (5MPs) are thiol-specific, reversible bioconjugation reagents for cysteine-specific protein modification, that are commonly used for protein bioconjugation[1].
Altenusin shows markedly DPPH radical scavenging activities.
Bis-PEG6-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5[1].
Hydroxy-PEG4-(CH2)2-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG4-(CH2)2-Boc is extracted from patent WO2004008101A2 (compound 191).
PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer[1].
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
(E)-Cinnamamide, the less active isomer of Cinnamamide. Cinnamamide, a derivative of the plant secondary compound Cinnamic acid. Cinnamamide is effectiveness as a non-lethal chemical repellent suitable for reducing avian pest damage[1].
(((9H-Fluoren-9-yl)methoxy)carbonyl)-D-tyrosine is a tyrosine derivative[1].
SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM; has better pharmacokinetic properties than pyrvinium, attenuates the growth of such Apc mutant organoids with EC50 of 2.9 uM; decreases the viability of the WNT-dependent cell lines (EC50 = 132, 63, and 123 nM for HT29, SW403, and HCT116 cells, respectively), inhibits the growth of CRC xenografts in mice; also attenuates the growth of patient-derived metastatic CRC xenograft, with minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
H-D-Ala-D-Ala-D-Ala-D-Ala-OH is a substrate for D-aminopeptidase[1].
DNP-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Acibenzolar-S-methyl (ASM) is a plant resistance inducer that mimics pathogen-host interactions and leads to systemic acquired resistance in plants. Acibenzolar-S-methyl helps reduce the use of pesticides and can be used in research to prevent plant diseases[1][2].
Lenumlostat is a Lysyl Oxidase Like 2 (LOXL2) inhibitor with an IC50 value <300 nM. Lenumlostat also exhibits antifibrotic activity[1][2].
PF-04447943 is a potent inhibitor of human recombinant PDE9A (IC50=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC50>1000 nM).
Azimsulfuron (DPX-A8947) is a sulfonylurea herbicide useful in controlling weeds in paddy fields[1].
Tetrahydrocortisone acetate is a intermediate product for production of tetrahydrocortisone 3-glucuronide[1].
N6-Ethyl-2’-C-methyladenosine 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].
Antiproliferative against-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative against-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative against-7 can increase ROS production and induce apoptosis[1].
DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects[1].
Lansoprazole Sulfide D4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacterium tuberculosis) agent with IC50 values of 0.59 µM intracellularly and 0.46 µM in broth[1].
(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)[1].
Raddeanoside R16 is an oleanane-type saponin, that can be isolated from the rhizoma of Anemone raddeana[1].
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) by tightly binding with it. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity[1].