Hsp90-IN-44 (compound 16) is a Hsp90 inhibitor with an IC50 of 9.8 µM. Hsp90-IN-44 can be used for cancer research.

HSP90-IN-28 (compound 12 h) is a potent and selective Hsp90 inhibitor with an IC50 of 0.46 μM for Hsp90α. HSP90-IN-28 exhibits ~48 fold selectivity versus other Hsp90β (IC50 = 22.28 μM).

HO 221 is an orally active benzoylphenylurea derivative with antitumor activity. HO 221 can inhibit the activity of mammalian DNA polymerase alpha. HO 221 can induce G1 phase arrest. HO 221 can be used for the research of cancer, such as leukemia.

HIV-1-IN-88 (compound 20a) is a potent HIV‑1 protease inhibitor (IC50 = 10 pM) with an antiviral EC50 of 10.4 nM. HIV-1-IN-88 exhibits potency against the multidrug-resistant variants HIV-1Muta and HIV-1I50V with EC50 values of 30.0 and 34.3 nM, respectively. HIV-1-IN-88 can be used for HIV research.

HIV RT-IN-1 is an inhibitor of HIV integrase and HIV reverse transcriptase-associated ribonuclease H. HIV RT-IN-1 is applicable to research related to HIV-1 infection.

HIF-PHD-IN-5 (Compound A4) is a hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) inhibitor. HIF-PHD-IN-5 can be used for the research of neurological disease.

Hexaprofen is a 2-arylpropionic acid derivative. Hexaprofen inhibits CXCL8-induced chemotaxis, while no activity is detected against CXCL1-induced chemotaxis.

HDAC-IN-97 is a PROTAC HDAC6 degrader-6that can be used for synthesis of PROTACs, such as HDAC6 degrader-6. HDAC6 degrader-6 is a potent HDAC6 PROTAC degrader with anticancer activity.

HDAC-IN-95 (Compound 9) is a HDAC inhibitor. HDAC-IN-95 can be used for the study of non-small cell lung cancer (NSCLC).

HDAC6-IN-78 (Example 48) is a selective HDAC6 inhibitor with an IC50 of 24 nM. HDAC6-IN-78 shows no activity against other HDAC isoforms.

GW694481 is an ApoA1 upregulator with IC50 values of 2.1 μM for CYP2C9 inhibition and 17.0 μM for CYP3A4 inhibition. GW694481 upregulates ApoA1 expression in human hepatic cells.GW694481 can be used for the research of atherosclerosis.

GS-1291269 is a potent and neutral ketohexokinase (KHK) inhibitor, with IC50s of 0.38 and 2.1 nM against KHK-C and KHK-A, respectively. GS-1291269 demonstrates liver and kidney fructose-1-phosphate (F1P) reduction in a fructose challenge model in rats. GS-1291269 can be used for kidney disease and metabolic-dysfunction-associated steatotic liver disease (MASLD) research.

GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer. (Pink: Estrogen Receptor/ERR ligand ; Blue: IAP ligand ; Black: linker).

GNE-3565 is an arylsulfonamide class NaV1.7 inhibitor with subnanomolar channel blockage and mixed subtype selectivity.GNE-3565 can be used for the research of pain.

Glucagon receptor antagonist-10 (Compound 11) is a glucagon receptor antagonist with a pIC50 of 7.154. Glucagon receptor antagonist-10 can be used in studies of glucose homeostasis.

Gentamicin B (SCH-14342) is an aminoglycoside antibiotic that can be isolated from Micromonospora echinospora. Gentamicin B can be used for the research of ataxia potential and renal toxicity.

GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases.

Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235  μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant.

Fmoc-C-PEG3-C3-Succinamic acid is a PROTAC linker that can be used in the synthesis of PROTACs.

Fluorofelbamate, a Felbamate analog, is a potent NMDA receptor antagonist. Fluorofelbamate exhibits anticonvulsant and antiepileptogenic effects in an experimental rat model of self-sustaining status epilepticus (SSSE). Fluorofelbamate can be used for epilepsy research.

FCH-2296413 is a potent and selective hydroxycarboxylic acid receptor (HCAR) agonist with an EC50 of 4.4-8.6 nM. FCH-2296413 exhibits analgesic activity and can be used for the research of peripheral pain-related diseases.

EVs inducer-1 is a release inducer of immunostimulatory extracellular vesicles (EVs). EVs inducer-1 inhibits tubulin polymerization. EVs inducer-1 enhances the release of immunostimulatory EVs by antigen-presenting cells, increases the release of EV particles from dendritic cells, and elevates CD63 reporter gene activity. EVs inducer-1 inhibits the viability of proliferating cells. EVs inducer-1 is applicable for research related to immune regulation.

Ethyl 4-(piperazin-1-yl)benzoate is a PROTAC linker that can be used in the synthesis of PROTACs.

EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.

EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAFV600E kinase inhibitor with human IC50 values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAFV600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAFV600E, including hydrogen bonding with EGFR Met769 and BRAFV600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer.

E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis.

E3 Ligase Ligand-linker Conjugate 225 is an E3 ligase ligand-linker conjugate used for the synthesis of PROTACs; it consists of the PEG-based linker Bis-Tos-PEG3 and the VHL-type E3 ubiquitin ligase ligand VH 101 thiol. E3 Ligase Ligand-linker Conjugate 225 can be further coupled with a target protein ligand—such as MT-4—to synthesize the PROTAC TG2 Degrader-3.

E3 Ligase Ligand-linker Conjugate 215 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 215 can be used to synthesize STAT3 PROTAC Degrader S3D5.

MW-436 (E 0471) hydrochloride is a benzofuran compound with antiarrhythmic effects. MW-436 hydrochloride can be used for the research of cardiovascular disease.

DU172 is a ligand for the adenosine A1 receptor (Adenosine A1 Receptor), with an IC50 of 24.9 nM against A1AR and an IC50 of 0.42 μM against A2AAR.