Potent, orally active and S1P3-sparing S1P1 agonist

Novel Selective Histone Deacetylase 6 (HDAC6) Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

Novel VISTA (V-domain immunoglobulin suppressor of T-cell activation) agonist

NPY5RA972 is a neuropeptide Y Y5 antagonist.

Novel modulator of Hydra head regeneration, inducing a homeotic transformation in Hydra

HAT Inhibitor II is a novel p300/CBP-selective histone acetyltransferase inhibitor.Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5µM; Histone Acetyltransferase Inhibitor II can be used in cancer research.

CID 2745687 is a competitive, reversible antagonist of the orphan receptor GPR35.

SGC2085 is a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.

4'-fluorouridine (4'-FlU, EIDD-2749) is a ribonucleoside analog that inhibits respiratory syncytial virus (RSV), related RNA viruses, and SARS-CoV-2 with high selectivity index (EC50/CC50 of ≥1877) in cells and human airway epithelia organoids. 4'-FlU induces a delayed stalling of RSV and SARS-CoV-2 RdRP (RNA-dependent RNA polymerase).

RH01687 is a small molecule that protect pancreatic β cells against endoplasmic reticulum stress-induced cell death.

LP99 is the first potent and selective BRD7/9 bromodomain inhibitor with Kd of 99 nM for BRD9.

GSK106 is a negative control compound used in binding and functional assays for PAD4 inhibitors.

B3C is an activator of transcription factor MEF2D; Enhabcer of cognitive capacity; Blocker of N-methyl-D-aspartate receptors.

Mesdopetam (IRL790) is an orally active and low toxicity dopamine D3 receptor antagonist. Mesdopetam can be used for the research of Parkinson's disease (PD).

DCN10809, also known as Paclitaxel succinate NHS ester, is a paclitaxel derivative with a succinic acid linker, in which the carboxy group is activated with an NHS ester. The NHS ester group is highly reactive to amino group or hydroxy group, and can be used to conjugate with other molecules such as peptides, proteins, antibodies or enzymes, or polymers. Paclitaxel-Succinic acid is a useful agent to make Paclitaxel-conjugate for drug delivery, nanodrug research.

Azvudine (RO 0622) is a potent HCV NS5B RNA polymerase inhibitor, inhibits HCV replication in the replicon system with IC50 of 24 nM; inhibits RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations (IC50=10-100 nM).

Vazegepant is the first intranasal CGRP receptor antagonist for the study the acute research of migraine.

Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease.

MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.

AZD7507 (AZD-7507) is a potent, selective, orally available CSF-1R (c-FMS) with IC50 of 32 nM.

MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.

Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity.

Rebamipide mofetil is an orally active prodrug of Rebamipide (OPC12759). Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner.

MAP4K4-IN-17 is a potent and highly selective MAP4K4 inhibitor with IC50 of 14.9 nM, showes improved overall drug-like properties compared to PF-06260933.

Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes alpha-synuclein protein (IC50=1.5 uM). Synucleozid selectively targets the alpha-synuclein mRNA 5? UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson's disease[1]. IC50 & Target: IC50: 1.5 uM (SNCA IRE RNA)[1] In Vitro: Synucleozid (0.25-1 uM; 24 hours) abrogates cytotoxicity induced by alpha-synuclein preformed fibrils, which act as seeds and recruit endogenous alpha-synuclein to aggregate[1]. Synucleozid (0-1 uM; 24 hours) binds to the A bulge near the base of the IRE hairpin, reduced levels of alpha-synuclein in a dose-dependent manner with an IC50 of 500 nM, and inhibits alpha-synuclein protein expression in SH-SY5Y neuroblastoma cells[1]. Synucleozid (100 nM-100 uM; 24 hours) binds to 2-AP-labeled and native IRE RNA with similar affinities. It decreases 2-AP emission with an EC50 value of 2.7 uM, recovery of 2-AP emissions is observed as a function of unlabeled SNCA IRE RNA (RNA-0) concentration, affording a competitive Kd of 1.5 uM[1]. Synucleozid (0.25-1 uM; 24 hours) decreases alpha-synuclein and other proteins that have IREs in their mRNA's UTR including APP, PrP, Ferritin and TfR as a dose-dependent mannner. All panels is completed in SH-SY5Y cells, except for PrP protein which is assessed in Neuro-2A cells[1].

MK-8591 (Islatravir, MK8591, EFdA) is a nucleoside analog that exhibits remarkable potency against wild-type and drug-resistant HIVs, inhibits HIV-1 reverse transcriptase with multiple mechanisms.

AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.

Nacubactam (OP 0595, RG 6080, RO 7079901) is a diazabicyclooctane that inhibits class A and C β-lactamases with IC50 of <1 uM, also acts as a PBP2-active antibacterial.

2BAct (eIF2B activator 2BAct) is a novel, highly selective, CNS-permeable small molecule eIF2B activator with EC50 of 33 nM in cell-based reporter assays.

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with potent anti-tumor activity.