Enozertinib (ORIC-114) hemihydrate is the inhibitor for EGFR that exhibits antineoplastic activity.

EGFR Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for EGFR and a PROTAC linker, which recruits E3 ligases. EGFR Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC EGFR degrader 3.

EN1033 is a covalent Immune regulatory transcription factor 5/8 (IRF5/8) degrader. EN1033 destabilizes and degrades IRF5 and IRF8 by covalently targeting cysteine residues C28 and C223, respectively, inhibiting their pro-inflammatory transcriptional activity, such as the reduced mRNA level of IL1A, IL1B and CCL2. EN1033 can be used for autoimmune and inflammatory diseases research.

PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry.

LXH-3-71 is a potent molecular glue PHGDH degrader. LXH-3-71 forms a dynamic chimera between PHGDH and the DDB1-CRL E3 ligase. LXH-3-71 modulates the stemness of colorectal cancer cells (CRCs) both in vitro and in vivo. LXH-3-71 can be used for colorectal cancer research.

ALOX5 stabilizer-1 is an arachidonate 5-lipoxygenase (ALOX5) stabilizer with a Kd of 7.26 μM. ALOX5 stabilizer-1 inhibits β-catenin protein levels and then suppresses STAT3 signal pathway. ALOX5 stabilizer-1 induces lung cancer cells apoptosis, inhibited cell migration and proliferation. ALOX5 stabilizer-1 can used for the study of non-small cell lung cancer (NSCLC).

CDRI-97/78 is an antimalarial agent. CDRI-97/78 has phototoxicity and can induce cell apoptosis and G2/M phase arrest. CDRI-97/78 can be used for the research of infection.

ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations.

RJW103 is a selective steroidogenic factor-1 (SF-1, NR5A1) agonist with a pEC50 of 6.5. RJW103 shows a pEC50 of 5.9 for liver receptor homologue-1 (LRH-1, NR5A2). RJW103 can be used for the researches of cancer, endocrinology and metabolic disease, such as adrenal cortex neoplasms.

[Ru(dpp)(bpy)(mtmp)](PF6)2 (Compound 5) is a trisheteroleptic ruthenium complex. [Ru(dpp)(bpy)(mtmp)](PF6)2 has a light-activated anticancer activity. [Ru(dpp)(bpy)(mtmp)](PF6)2 can selectively cleave off upon green light irradiation, thereby releasing a phototoxic ruthenium-based photoproduct that binds to nuclear DNA, induces DNA damage and apoptosis in cancer cells. [Ru(dpp)(bpy)(mtmp)](PF6)2 can be used for phototherapy of cancers like conjunctival melanoma research.

JNJ-17166864 is a highly selective CCR2 antagonist. JNJ-17166864 has low oral bioavailability. JNJ-17166864 can significantly reduce the area of alveolar bone loss in a mouse model of periodontitis induced by Porphyromonas gingivalis infection. JNJ-17166864 can be used in the research of inflammatory diseases such as allergic rhinitis and periodontitis.

SM (d18:1/15:0) is a sphingomyelinase inhibitor. SM (d18:1/15:0) is promising for research of neurodegenerative diseases (e.g., Alzheimer's) and metabolic syndrome.

(S)-Edelfosine ((S)-ET-18-OCH3) is the (S)-enantiomer of Edelfosine (ET-18-OCH3). Edelfosine is a selective antitumour lipid targeting apoptosis through intracellular activation of Fas/CD95 Death receptor.

SDZ-CPI-975 is a novel, reversible, and selective CPT I inhibitor. SDZ-CPI-975 effectively inhibits fatty acid oxidation and lowers blood glucose levels.

AR ligand-44 TFA is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051.

AR ligand-44 is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051.

mrt-5702D is a molecular glue degrader targeting cereblon (CRBN). mrt-5702D forms a CRBN-MRT-5702D-G3BP2 ternary complex to activate the ubiquitin-proteasome system for G3BP2 degradation. mrt-5702D is promising for research of G3BP2-related cancers (e.g., breast cancer, lung cancer) and neurodegenerative diseases.

Angustilongine M is a microtubule-targeting antitumor alkaloid (IC50=0.2 μM against HT-29 cells). Angustilongine M induces G0/G1 cell cycle arrest and mitochondrial apoptosis via tubulin polymerization promotion. Angustilongine M is promising for research of colorectal cancer and other solid tumors.

BAL-0019764 is an iron carrier monocyclic β-lactam with broad-spectrum β-lactase inhibition ability. BAL-0019764 has inhibitory activity against various Gram negative bacteria. BAL-0019764 is commonly used in the study of bacterial infections.

Z52/Z56 intermediate is a key intermediate in the synthesis of RAS inhibitors.

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with KD values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy.

BIRT2584 is an LFA-1 inhibitor. BIRT2584 can be used for research on autoimmune diseases.

Tisolagiline (KDS2010) methylsulfate is the selective, reversible and orally active inhibitor for MAO-B with an IC50 of 8 nM. Tisolagiline methylsulfate exhibits neuroprotective and anti-neuroinflammatory activities.

BMS-279700 is an orally active Src-family kinase p56Lck inhibitor. BMS-279700 can block the production of proinflammatory cytokines (IL-2 and TNFα). BMS-279700 can inhibit T cell proliferation. BMS-279700 can be used for the researches of inflammation and immunology.

Topoisomerase inhibitor 6 (Compound REDX05931) is a dual irreversible inhibitor of DNA gyrase and topoisomerase IV (MIC=0.06 μg/mL against fluoroquinolone-resistant S. aureus). Topoisomerase inhibitor 6 blocks DNA strand break-reunion, inducing lethal DNA damage. Topoisomerase inhibitor 6 is promising for research of Gram-positive bacterial infections (e.g., S. aureus, S. pneumoniae).

Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.

(R)-ACE-OH is the enantiomer of (S)-ACE-OH.

(R)-PHA533533 is an inactive enantiomer (S)-PHA533533 (active enantiomer). (S)-PHA533533 is a CDK2 inhibitor with antitumor activity.

SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research.

A-75998 is an antagonist of luteinizing hormone-releasing hormone (LHRH). A-75998 can be used in the research of diseases such as hormone-sensitive cancers and endometriosis.