Nalfurafine (TRK-820, TRK820) is potent, selective agonist of kappa-opioid receptor with Ki of 3.5 nM, 15-fold less potent for μOR and little affinity for δOR (Ki=53 and 1,200 nM, respectively).It is for research use only, and the end user must be the universities.

Fraisinib is a specific and effective inhibitor of glycyl-tRNA synthetase 1 (GARS1), suppresses the synthesis of Ap4A by GARS1 and displays strong anti-tumoral potential.

SPI-21 (Spt5-Pol II inhibitor 21) is a small-molecule inhibitor of Spt5-Pol II with IC50 of 25.2 uM.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

Onvansertib, also know as NMS-P937, PCM-075 and NMS1286937, is an oral Polo-like kinase 1 (PLK1) inhibitor, a key regulator of cell cycle progression and mitosis. It selectively inhibits PLK1 with a reported half-maximal inhibitory concentration (IC₅₀) of approximately 2 nM, while demonstrating significantly lower activity against other Polo-like kinases (PLK2 and PLK3). Onvansertib has shown potent anti-proliferative effects in various cancer cell lines, particularly in colorectal cancer, acute myeloid leukemia (AML), and prostate cancer models. It induces mitotic arrest, leading to apoptosis in tumor cells. Onvansertib has demonstrated synergistic effects when combined with chemotherapeutics such as irinotecan, 5-fluorouracil (5-FU), and decitabine, enhancing their efficacy in resistant cancers.

Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.

Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity(IC50=1.2 nM).

S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively.

F1957-0088 is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (TTD vs. H3K9me3) EC50 of 45.1 uM.

ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A.

Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.

Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease[1][2].

LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.

KRCT-6j is a potent and selective TYRO3 inhibitor, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated cell migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.

NADI-351 is a specific small-molecule inhibitor of Notch1 transcriptional complexes with IC50 of 8.8 uM in cellualr reporter assays.NADI-351 inhibited OE33 cell growth in single dose MTT assays (EC50= 10 uM) and, more potently, in multi-dose colony formation assays (EC50=1.3 uM)NADI-351 is 15 times more potent than IMR-1 in an NTC AlphaScreen assay.NADI-351 selectively disrupted Notch1 transcription complexes, inhibited recruitment of Notch1 to the NTC (Notch Ternary Complex) and to the HES1 promoter, and reduced Notch1 recruitment to target genes.NADI-351 inhibits tumor growth in Notch-dependent cancers and does not exert gastrointestinal toxicity associated with goblet cell metaplasia.NADI-351 selectively inhibits stem-like esophageal adenocarcinoma (EAC) cell populations.

(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).

RBI2 (Ribosome biogenesis inhibitor 2) is a small molecule inhibitor of ribosome biogenesis inhibitor, potently inhibits pre-rRNA levels in A375 with IC50 of 169 nM.

Pyrcoumin is a competitive inhibitor of dCTP pyrophosphatase 1 (dCTPP1, IC50=3.3 uM), inhibits Wnt signaling with IC50 of 8.4 uM in SuperTOPFlash reporter gene assays.

A potent and selective Histamine H3 receptor antagonist with Ki of 0.1-5.8 nM (human, rat H3).

Maltopentaose is the shortest chain oligosaccharide that can be classified as maltodextrin and is also used in a study to investigate glycation and phosphorylation of α-lactalbumin.

Fluorescein-5-maleimide is a fluorescent thiol-reactive dye used to conjugate fluorescein to proteins (excitation: 494 nm, emission: 519 nm).

GSK137 is a potent, small-molecule BCL6 inhibitor binding to BCL6 BTB-POZ domain, displaces peptides derived from the human SMRT co-repressor from the BCL6 BTB-POZ domain in a TR-FRET assay with a pIC50 of 8.0.

MitoBloCK 1 is a small molecule inhibitor that blocks the import of substrates that use the TIM22 import pathway, but not TIM23 or the Mia40/Erv1 translocation pathways.

Potent and selective nociceptin opioid receptor (NOP) agonist

AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the active HER2-HER3 heterodimer, inhibits oncogenic downstream signalling in SK-BR-3 breast cancer cells.

Galvestine-1 is a potent small-molecule inhibitor of monogalactosyldiacylglycerol (MGDG) synthase that competitively binds to the diacylglycerol substrate site with an IC50 of 10 μM. This bioactive compound demonstrates excellent plant mobility, being efficiently absorbed through roots and systemically distributed via xylem transport to mesophyll tissues. In Arabidopsis thaliana, Galvestine-1 treatment leads to significant reduction of MGDG content and disrupts chloroplast development, likely through impairment of thylakoid membrane biogenesis. These unique properties establish Galvestine-1 as a valuable chemical tool for investigating MGDG-dependent processes and studying lipid homeostasis mechanisms in plants.

AC-003 is a novel, orally administered small-molecule inhibitor targeting receptor-interacting protein kinase 1 (RIPK1), demonstrating therapeutic potential for the treatment of idiopathic pulmonary fibrosis (IPF).

YJ9069 is a potent, selective and orally bioavailable PROTAC degrader of CDK12/CDK13. It inhibits proliferation in prostate cancer cells by inducing gene-length-dependent transcriptional elongation defects, leading to DNA damage, cell-cycle arrest, and significant tumor growth suppression in vivo.

Pranlukast hemihydrate (ONO-1078 hemihydrate) is an antagonist of cysteinyl leukotriene receptor-1 (CysLT1) that blocks leukotrienes such as LTC4, LTD4, and LTE4, reducing bronchoconstriction and airway inflammation. It also inhibits NF-κB activation, thereby suppressing proinflammatory cytokine production (e.g., IL-6, IL-1, TNF-α) in monocytes/macrophages and T cells, contributing to its immunomodulatory effects.

Duocarmycin SA is a potent antitumor antibiotic with an IC50 of 10 pM. It is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA and can be used in research treatment for glioblastoma multiforme (GBM).