Butenafine is a potent and broad spectrum benzylamine antifungal agent[1]. Butenafine inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation, leading to a deficiency of the fungal cell membranes. Butenafine is effective against dermatophytes infections, such as tinea pedis, tinea cruris, tinea versicolor[1][2].
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].
Metixene hydrochloride hydrate is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM[1].
Deacetyl Ganoderic Acid F is a 7-anostane triterpenoid from Ganoderma lucidum.
Glycoside St-J (Compound 2) is a triterpenoid saponin. Glycoside St-J has antitumor activity and inhibits HeLa cell proliferation. Glycoside St-J Isolates from natural Anemone flaccida. Glycoside St-J can be used in the development of new anticancer agents [1].
Obestatin(human) is an endogenous peptide derived from the same prepropeptide as ghrelin. Obestatin(human) suppresses food intake and reduce body weight-gain in rats.
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].
H-Lys-Arg-OH is a biologically active peptide.
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].
PD 125967 is an oligopeptide renin inhibitor. PD125967 can be used to low blood pressure[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].
5-carboxypentan-1-olate-d6 (sodium) is the deuterium labeled Sodium 5-carboxypentan-1-olate[1].
Sethoxydim is a postemergent herbicide. Sethoxydim inhibits plant acetyl-coenzyme A carboxylase (ACCase) activity[1][2].
Methopterin inhibits osteoclasts proliferation. Methopterin inhibits the activation and bone resorption function of osteoclasts, and induced osteoclasts apoptosis[1].
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.
L-Isoleucine β-naphthylamide is an isoleucine derivative[1].
N-Acetyl-S-(2-cyanoethyl)-L-cysteine-d3 is the deuterium labeled N-Acetyl-S-(2-cyanoethyl)-L-cysteine[1].
Fmoc-Sar-OPfp is a Glycine (HY-Y0966) derivative[1].
Cetraxate is an orally active antiulcer Drug. Cetraxate increases the blood flow of gastric mucosal. Cetraxate increases the eradication of Helicobacter pylori in smokers when in combination with Omeprazole (HY-B0113),Amoxicillin (HY-B0467A), and Clarithromycin (HY-17508) [1].
HUP30 is a vasodilating agent. HUP30 stimulates soluble guanylyl cyclase, activate K+ channels, and blocks extracellular Ca2+ influx[1].
DL-3-Phenylserine hydrate is a serine derivative[1].
Benzyloxycarbonyl-D-alloisoleucine is an isoleucine derivative[1].
Sanggenol A acts as a dual inhibitor of nitrofuranone reduction mediated by the intestinal microbial nitrification reductases EcNfsA and EcNfsB. In addition, Sanggenol A is also an effective inhibitor of intestinal bacterial β-glucuronidase[1].
MV1035 (MV-1035) is a novel small molecule that reduce U87 GBM cells migration and invasiveness, targeting m6A demethylase ALKBH5, also inhibits ALKBH2;MV1035 directly inhibits active recombinant ALKBH5 protein and, consequently, negatively regulates CD73 protein expression without affecting CD73 mRNA transcription.In PD-GSCs, MV1035 has a synergistic effect with TMZ in reducing cell viability and their ability to form spheres.MV1035 is able both to reduce the expression of MGMT and to inhibit ALKBH2 activity.