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).

CVT-10216 is a potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50 values are 29 and 1300 nM for ALDH2 and ALDH1, respectively).

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.

Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

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.

LY3499446 (KRASG12C IN-13) is a potent inhibitor of KRAS G12C. It can be used in research on advanced solid tumors, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).

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).

BBI-355 is an oral, potent, and selective small molecule inhibitor of CHK1 with an IC50 of 0.3 nM. It demonstrates significant anti-tumor activity as a single agent and in combination with targeted therapies in multiple ecDNA+ oncogene amplified tumor models.

Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.

α-Lipoic Acid Derivative 1 (Compound AN-7) is an α-lipoic acid derivative that enhances glucose transport in skeletal muscle by releasing active α-lipoic acid (LA), significantly improving glucose metabolism. In L6 skeletal muscle cells, α-Lipoic Acid Derivative 1 significantly increases glucose transport rates, approximately 12 times more potent than the parent compound α-lipoic acid. In a mild diabetic mouse model, 10 mg/kg of α-Lipoic Acid Derivative 1 administered for two weeks significantly reduced blood glucose levels by 39%. α-Lipoic Acid Derivative 1 shows significant potential in research related to glucose metabolism in diabetes.

ZYH-23 is a potent necroptosis inhibitor. ZYH-23 blocks necroptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation via HSP90 targeting.

ZPD-2 inhibits the aggregation of C-terminally truncated and full-length α-synuclein. ZPD-2 inhibits the formation and fibrillation of α-Syn, thereby preventing its propagation. ZPD-2 can be used in research of Parkinson's disease.

ZM522 is a CD73 inhibitor with an IC50 value of 0.56 μM. ZM522 effectively increases the levels of interferon-γ (INF-γ) and enhances immune activity by regulating the activation status of T cells. ZM522 holds promise for research in the fields of immunology and cancer therapy.

ZK-316 is a potent and broad-spectrum NNRTI inhibitor with an EC50s ranging from 0.99 to 75.1 nM. ZK-316 can be used in the study of HIV.

ZINC00230567 is an inhibitor for Lipocalin-2 (LCN2). ZINC00230567 reduces the colony formation and cell viability of cell SUM149, and exhibits anti-tumor efficacy.

ZHAWOC8655 is a USP18 inhibitor. ZHAWOC8655 compromises cellular USP18/ISG15 binding and inhibits USP18 protease activity in vitro.