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IND 100 Publications

PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon

Poly ADP-ribose polymerases (PARPs) are a family of enzymes related to DNA damage repair process. Inhibition of PARP1/2 accelerates the damage of injured DNA, which is synthetically lethal to DNA-repairing-deficient cancer cells, such as BRCA1/2-deficient cells. PARP1/2 inhibitors could be a promising candidate for the treatment of cancer. The PARP1 and PARP2 inhibition assays were performed by Medicilon.

PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon

Discovery of STAT3 and HDAC dual-pathway inhibitors for the treatment of solid cancer. The PK experiment in SD Rats was carried out by Medicilon

The inhibition of HDACs will lead to compensated activation of a notorious cancer-related drug target, STAT3, in breast cancer through a cascade, which probably limits the anti-proliferation effect of HDAC inhibitors in solid tumors. Herein, researchers synthesized a series of potent pterostilbene hydroxamic acid derivatives with dual-target inhibition activity. The pharmacokinetic experiment in SD Rats was carried out by Medicilon.

Discovery of STAT3 and HDAC dual-pathway inhibitors for the treatment of solid cancer. The PK experiment in SD Rats was carried out by Medicilon

Apatinib inhibits Paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway

Overexpression of VEGFR2 can offset the rescue effect of Apatinib on Paclitaxel-induced drug resistance of MGC803 cells. Apatinib inhibits Paclitaxel resistance of MGC803 cells via the VEGFR2 signaling pathway. In this research, the VEGFR2 sequences were designed and then amplified by RT-PCR. The sequences were then ligated with a pcDNA3.0 plasmid to construct a recombinant pcDNA3.0-VEGFR2 vector (Medicilon).

Apatinib inhibits Paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway

Researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable

The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification of RNA. Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable, while its enantiomer UZH1b is essentially inactive. The authors thank Medicilon for the synthesis of the UZH1a and UZH1b compounds.

Researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable

Researchers designed and synthesized a photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies were conducted by Medicilon

Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades. In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies of compounds 1 and 2 were conducted by Medicilon. Medicilon's pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody.

Researchers designed and synthesized a photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies were conducted by Medicilon

RIPK2 is an enzyme involved in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase and demonstrates favorable in vitro ADME and PK properties. The PK study was conducted by Medicilon

Receptor interacting protein kinase-2 (RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase (IC50=8 nM) and demonstrates favorable in vitro ADME and pharmacokinetic properties. The pharmacokinetic study was conducted by Medicilon.

RIPK2 is an enzyme involved in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase and demonstrates favorable in vitro ADME and PK properties. The PK study was conducted by Medicilon

Syntheses, biological evaluations, and mechanistic studies of potent PD-L1 inhibitors with in vivo antitumor activity. PK studies were conducted by Medicilon

PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified compound L7 as a potent PD-L1 inhibitor that blocked PD-1/PD-L1 interaction. Pharmacokinetic (PK) studies demonstrated that L7 was orally bioavailable. PK studies were conducted by Medicilon.

Syntheses, biological evaluations, and mechanistic studies of potent PD-L1 inhibitors with in vivo antitumor activity. PK studies were conducted by Medicilon

SLL-1206 is a kappa opioid receptor agonist with substantially improved physicochemical and pharmacokinetic properties

The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects. The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.

SLL-1206 is a kappa opioid receptor agonist with substantially improved physicochemical and pharmacokinetic properties

Benzimidazole derivative XY123 is a potent, selective, and orally available RORγ inverse agonist. In this study, all liver microsome assays were performed by Medicilon

Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. XY123 potently inhibits the RORγ transcription activity with an IC50 value of 64 nM. XY123 demonstrates good metabolic stability and a pharmacokinetics property with reasonable oral bioavailability (32.41%) and moderate half-life (4.98 h). All liver microsome assays were performed by Medicilon.

Benzimidazole derivative XY123 is a potent, selective, and orally available RORγ inverse agonist. In this study, all liver microsome assays were performed by Medicilon

zapERtrap: A light-regulated ER release system reveals unexpected neuronal trafficking pathways. Synthesis of zapalog was performed by Medicilon

zapERtrap opens the door to previously unapproachable questions concerning how proteins are processed, trafficked, and secreted in space and time in complex cellular environments. zapERtrap relies on a small-molecule protein dimerizer zapalog, which consists of the antibiotic trimethoprim tethered to a synthetic ligand of FK506-binding protein through a photocleavable linker. Synthesis of Zapalog was performed by Medicilon.

zapERtrap: A light-regulated ER release system reveals unexpected neuronal trafficking pathways. Synthesis of zapalog was performed by Medicilon

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