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IND 100 Publications

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

Tankyrase 1/2 impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer

Tankyrase 1 and 2 (TNKS1/2) impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer. OM-153 shows picomolar IC50 inhibition in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable ADME properties, and an improved pharmacokinetic profile in mice. The pharmacokinetic analyses in mice were performed according to the standard protocols of Medicilon.

Tankyrase 1/2 impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer

Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon

Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Researchers designed 1-(Indolizin-3-yl)ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer. Pharmacokinetic properties evaluation were analyzed by Medicilon. Liver microsomal stability assay were performed at Medicilon. Caco-2 permeability assay was analyzed by Medicilon.

Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon

Researchers used RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. RZ-2994 was obtained from Medicilon

Despite progress in the treatment of T-cell acute lymphoblastic leukemia (T-ALL) has limited treatment options, particularly in the setting of relapsed/refractory disease. Researchers used SHMT1/2 inhibitor RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. Loss of both SHMT1/2 is necessary for impaired growth and cell cycle arrest, with suppression of SHMT1/2 inhibiting leukemia progression. RZ-2994 also decreases leukemia burden in vivo. RZ-2994 was obtained from Medicilon. Medicilon offers a full range of chemical services covering all phases of your project. Cus-tomers can work with us either through FFS or FTE.

Researchers used RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. RZ-2994 was obtained from Medicilon

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