[Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC50 of 7.24. [Orn5]-URP displays no agonist activity[1][2].
PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively[1].
Cassiachromone can be isoalted from Cassia siamea[1].
Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
N-(3-Nitro-2-pyridinesulfenyl)-L-glutamic acid γ-t-butyl ester is a glutamic acid derivative[1].
LysoTracker Red (LysoTracker Red DND-99) is a paraformaldehyde fixable probe that concentrates into acidic compartments of cells and tissues. LysoTracker Red is an indicator of cell death in a manner similar to other standard assays (Annexin, terminal dUTP nick end labeling, Nile blue sulfate, neutral red, and acridine orange)[1]. LysoTracker Red is a marker for late endosomes and lysosomes[2].
YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities[1].
(-)-Haplomyrfolin is a natural lignan with anticancer effects[1].
J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway[1].
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells[1]. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells[2].
Boc-D-Gly(allyl)-OH.DCHA is a Glycine (HY-Y0966) derivative[1].
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research[1].
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research[1].
2’-Deoxy-2’-fluoro-6-S-methyl-6-thio-arabino-inosine 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].
CT1113 is a potent USP28 and USP25 inhibitor. CT1113 decreases the MYC level in vivo，exhibits anti-tumor activity in mouse pancreatic cancer CDX model[1].
10-Hydroxyaloin B is a bioactive oxanthrone based on the aloin skeleton[1].
Cuniloside B (Eucalmaidin E) is a non-volatile glucose monoterpene ester. Cuniloside B can be used as a fragrance additive[1].
SMER28 is an autophagy activator acting via an mTOR-independent mechanism. SMER28 prevents the accumulation of amyloid beta peptide.
Dynamin IN-1 is a potent dynamin inhibitor with an IC50 value of 1.0 µM[1].
Sulfadimethoxine is a sulfonamide antibiotic.Target: AntibacterialSulfadimethoxine is a sulfonamide antibiotic. Sulfadimethoxine is used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections. It is most frequently used in veterinary medicine, although it is approved in some countries for use in humans. Sulfadimethoxine inhibits bacterial synthesis of folic acid (pteroylglutamic acid) from para-aminobenzoic acid. Sulfadimethoxine is approved in Russia for use in humans, including children, and has been successfully used there for more than 35 years. It is widely available in Russia as an over-the-counter drug manufactured by a number of Russian pharmaceutical companies [1].
Sethoxydim is a postemergent herbicide. Sethoxydim inhibits plant acetyl-coenzyme A carboxylase (ACCase) activity[1][2].
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646)Target: EZH2 inhibitorIn vitro: EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
N-Acetyl-S-(2-cyanoethyl)-L-cysteine-d3 is the deuterium labeled N-Acetyl-S-(2-cyanoethyl)-L-cysteine[1].
HUP30 is a vasodilating agent. HUP30 stimulates soluble guanylyl cyclase, activate K+ channels, and blocks extracellular Ca2+ influx[1].
2,7-Dihydrohomoerysotrine is an alkaloid that can be found in Dysoxylum[1].
DSPE-PEG(2000)-Amine is used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents[1][2][3].
PI4K-IN-1 (compound 44) is a potent PI4KIII inhibitor, with pIC50 values of 9.0 and 6.6 for PI4KIIIα and PI4KIIIβ, respectively. PI4K-IN-1 also inhibits PI3Kα/β/γ/δ, with pIC50 values of 4.0/<3.7/5.0/<4.1, respectively[1].
DNA Gyrase-IN-3 (Compound 28) is a bacterial DNA gyrase B inhibitor with IC50s of 5.41-15.64 µM for E. coli DNA gyrase. Anti-tubercular and antibacterial activity[1].
Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl. Desacetyl bisacodyl induces epithelial Cl(-) secretion in rat colon and rectum. Desacetyl bisacodyl evokes several effects at the colon or rectum, including increased mucus and chloride secretion[1].