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.

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.

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.

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].

CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

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).

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

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.

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.

ZG297 is an agonist for Staphylococcus aureus ClpP (SaClpP ) with an EC50 of 0.26 μM. ZG297 degrades SaFtsZ, inhibits the bacterial cell division, thereby exhibiting antistaphylococcal activity, that inhibits S. aureus 8325-4 strains and MRSA strains with MIC of 0.063-256 μg/mL. ZG297 exhibits anti-infectious efficacy in mouse models.

Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.

Z-CITCO is the cis isomer of CITCO and a selective ligand for the anti-estrogen binding site (AEBS), the binding affinities (Ki) of PBPE hydrochloride and MBPE to AEBS are 8.79 and 17.57 nM, respectively.

Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptor X2) with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC50 values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions.