PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity[1].
Pronase E is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
C6 NBD Lactosylceramide is a derivative of lactosylceramides, and can be used in lactosylceramide synthase assay as a fluorescent acceptor substrate. C6 NBD Lactosylceramide can also be used in cancer research[1][2].
OptoBI-1 is a photochromic TRPC3 agonist, which asts as a photopharmacological tool to control of neuronal firing[1].
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent ROR isoforms selectivity (>5000-fold selectivity against human RORα and RORβ)[1].
Novel inhibitor of ER-to-cytosol protein dislocation, exhibiting anti-dengue and anti-Zika virus activity
E3 ligase Ligand-Linker Conjugates 7 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
A small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo; also reversibly attenuates fine touch perception in normal mice, reverses pathological mechanical hypersensitivity.
Fmoc-D-Pro-OH is a proline derivative[1].
Cdk5 Substrate is a biological active peptide. (substrate for the cdc2 protein kinase)
Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases[1].
Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP[1][2].
LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitors of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production[1].
MurA-IN-2 (compound 37), a chloroacetamide fragment containing a primary aliphatic amine, is a potent MurA inhibitor with an IC50 value of 39 μM. MurA-IN-2 has antibacterial activity and inhibits the bacterial cell wall synthesis[1].
P-T-P-S-NH2 is a short-chain peptide with an N-terminal proline[1].
TC11 is a MCL1 degradator and Caspase-9 and CDK1 activator. TC11 structurally relates to immunomodulatory drugs as phenylphthalimide derivative. TC11 induces apoptotic death caused by degradation of MCL1 during prolonged mitotic arrest[1][2].
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research[2].
SARS-CoV-2 nsp13-IN-5 (compound C6) is a potent SARS-CoV-2 nsp13 inhibitor with IC50 values of 50 and 55 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-5 can be used for researching anti-COVID-19[1].
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3].
Hygric acid (N-Methyl-L-proline) is a proline analogue found in the citrus juices and the juice of bergamot[1].
Trans-Trimethoxyresveratrol is a derivative of Resveratrol (RSV),and it may be a more potent anti-inflammatory, antiangiogenic and vascular-disrupting agent when compared with resveratrol.In vitro: The in vitro study of resveratrol and trans-Trimethoxyresveratrol showed rather weak cytotoxic effects on three cancer cell lines (HepG2, MCF-7, and MDA-MB-231), which contradicted a previous study reporting that resveratrol inhibited MCF-7 cells with an IC50 of about 10?μM. This discrepancy might be explained by the fact that the measurements were made 24?h after drug treatment, whereas the measurements of the previous study were taken 6 days after. The fact that the cytotoxic effect of trans-Trimethoxyresveratrol was lower than that of resveratrol is surprising, because in many studies, trans-Trimethoxyresveratrol is the most active analogue of resveratrol , although resveratrol shows much stronger antioxidant effects than that of trans-Trimethoxyresveratrol.[1]In vivo: Zebrafish embryos offer great advantage over their adults as well as other in vivo models because of the external development and optical transparency during their first few days, making them invaluable in the inspection of developmental processes. These unique advantages can even be made more useful when specific cell types are labeled with fluorescent probes. Zebrafish embryo in vivo, suggests that trans-Trimethoxyresveratrol has both more potent antiangiogenic activity and more importantly, stronger specific cytotoxic effects on endothelial cells than does resveratrol.[1]
RBC6 is an inhibitor of GTPases RalA. RBC6 inhibits binding of Ral to its effector RALBP1. RBC6 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts, as well as anchorage-independent growth of human cancer celllines[1].
Azido-PEG3-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG3-maleimide is also a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Cionin is a disulfotyrosyl hybrid of cholecystokinin and gastrin[1].
MMP-9-IN-8 (Compound 3) is an MMP-9 inhibitor with inhibitory activities of 42.16% and 58.28% at 10 μM and 50 μM concentrations, respectively. MMP-9-IN-8 has anti-cancer activity and can induce apoptosis in MCF-7 cells with an IC50 value of 23.42 μM[1].
CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer[1].
Egg Laying Hormone, aplysia is a neuropeptide synthesized by the bag cell neurons, which contains 36 amino acids and can stimulate egglaying and ovulation in Aplysia via electrical discharge triggering of neurons. Egg-laying hormone of Aplysia induces a voltage-dependent slow inward current carried by Na' in an identified motoneuron[1][2].
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer[1].
Pomalidomide-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].