effect

Thiamphenicol (Dextrosulphenidol) is a methylsulfonyl analog of chloramphenicol. It is an antibiotic and immunosuppressive agent.

Castor oil (Xenaderm) is a vegetable oil pressed from the seeds of the castor bean, Ricinus communis, used as a laxative and as an excipient in medicinally.

Isotoosendanin ((1S,2S,4R,5S,6R,9S,10S,11R,13R,18S,20R)-20-(acetyloxy)-6-(furan-3-yl)-11,15,18-trihydroxy-5,10,14-trimethyl-3,8-dioxo-16-oxapentacyclo[12.3.3.01,13.02,1?.0?,?]icosan-4-yl acetate) is a limonoid isolated from Melia toosendan fruit with anti-inflammatory and analgesic capacity.

D18024 is a phthalazinonderivat with anti-allergic and anti-histamine effect.

Ceruletide is a decapeptide that serves as a safe and effective cholecystokinin receptor agonist, exerting a direct spasmogenic effect on the gallbladder muscle and bile ducts, and is commonly used to establish pancreatitis models.

PCO371 (2,4-Imidazolidinedione, 1-(3,5-dimethyl-4-(2-((4-oxo-2-(4-(trifluoromethoxy)phenyl)-1,3,8-triazaspiro(4.5)dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-5,5-dimethyl-) is an orally active full agonist of parathyroid hormone receptor 1. It has no effect on PTH type 2 receptor.

Trastuzumab deruxtecan (T-DXd) is an antibody-active molecule conjugate (ADC) with anticancer and antitumor activity, which is composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2) coupled to a topoisomerase I inhibitor (DXd). Trastuzumab deruxtecan has an improved effect on the treatment of HER2-positive breast cancer and gastric cancer.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

AFMK (Formyl-N-acetyl-5-methoxykynurenamine) is an active metabolite of Melatonin with antioxidant and free radical scavenging activity. AFMK is a modulator of apoptosis and improves the anti-tumor effect of Gemcitabine in PANC-1 cells.

Etomoxir is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that inhibits fatty acid oxidation by inhibiting CPT-1a and inhibits palmitate oxidation in humans, rats, and guinea pigs. Etomoxir has an inhibitory effect on adenine nucleotide translocase and can inhibit macrophage polarization by disrupting CoA homeostasis.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

Asperphenamate is a fungal metabolite of Aspergillus flatiipes. The IC50s for T47D cells, MDA-MB-231 cells, and HL-60 cells are 92.3 μM, 96.5 μM, and 97.9 μM. Asperphenamate shows an anticancer effect.

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

BI-2852 is a KRAS inhibitor targeting the switch I II pocket (SI II-pocket) with nanomolar affinity, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

CS-722 Free base is a synthetic central muscle relaxant exhibiting muscle relaxant effects and inhibition of spinal reflexes. In hippocampal cultures, CS-722 Free base may suppress spontaneous inhibitory and excitatory post-synaptic currents by inhibiting sodium and calcium currents.

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.

DB1976 is a selenophene analog of DB270 and a highly potent, cell-permeable, fully efficacious transcription factor PU.1 inhibitor. It effectively inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1 DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. Additionally, DB1976 has an apoptosis-inducing effect.

DSR-6434 is a selective agonist of TLR7 with antitumor effect. DSR-6434 exhibits EC50s of 7.2 nM and 4.6 nM for human and mouse.

GKI-1 is a Greatwall (GWL) kinase inhibitor with an IC50 of 4.9 for hGWLFL and 2.5 µM for hGWL-KinDom. It exhibits stronger inhibition on ROCK1 with an IC50 of 11 µM and only weakly inhibits PKA.

GKI-1 HCl is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL and hGWL-KinDom.The inhibitory effect of GKI-1 HCl on ROCK1 is more significant.

Guaiapate has an antitussive and sedative effect.

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor with a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, without affecting the nuclear translocation of p65 mediated by the TNF-α receptor. It inhibits p52 nuclear translocation stimulated by TWEAK or Anti-LTβR with an IC50 of 10 μM and regulates the NF-kB signaling pathway in a ligand-independent manner.

Oxaquin is an effective, water-soluble, injectable prodrug that is rapidly converted to the active substance MCB3681 after intravenous administration in the body. Oxaquin is active against Gram-positive bacteria, but has no antibacterial effect on its own.