HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTKC481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma.

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.

GSTO1-IN-5 is a potent and selective glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50of 0.22 nM. GSTO1-IN-5 can be used for the researches of cancer and inflammation, such as colon cancer.

GSK3-IN-11 is a Glycogen Synthase Kinase-3 (GSK-3) inhibitor with an IC50 of 5010 nM.

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.

GPX4-IN-21 (Compound 4d) is a selective glutathione peroxidase 4 (GPX4) inhibitor. GPX4-IN-21 can induce ferroptosis and downregulate the ferroptosis-related proteins SLC7A11, SLC11A2 and GPX4 levels. GPX4-IN-21 can induce ROS and MDA accumulation GPX4-IN-21 exhibits potent anti-proliferative activity. GPX4-IN-21 can be used for the research of cancer, such as melanoma.

GPX4-IN-19 is an effective GPX4 inhibitor (IC50 = 0.311 μM), covalently binds to the Sec 46 site of GPX4. GPX4-IN-19 shows strong anti-proliferative activity with high ferroptosis selectivity. GPX4-IN-19 causes intracellular Fe2+ accumulation, leading to increased levels of lipid peroxides (LPOs) and reactive oxygen species (ROS), which induces ferroptosis and subsequently results in DNA damage. GPX4-IN-19 can be used for the study of Triple-Negative Breast Cancer (TNBC).

GPR6 inverse agonist 1 (Compound 101) is a selective GPR6 inverse agonist with an IC50 < 100 nM. GPR6 inverse agonist 1 is applicable to research related to Parkinson's disease and Huntington's disease.

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.

Gd-PCTA-Ach is a macrocyclic gadolinium-based MRI contrast agent with high kinetic inertness and moderate albumin affinity. The albumin-binding property of Gd-PCTA-Ach effectively prolongs its blood circulation time. Gd-PCTA-Ach is mainly cleared via the kidneys, while approximately 10% of the dose is excreted through the hepatobiliary pathway, exhibiting a unique dual-channel excretion profile. Gd-PCTA-Ach enables high-quality imaging of brain and liver tumor lesions, and has important application value in diagnostic studies of liver cancer and glioma.

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.

FXR DUBTAC IN-1 (compound D11) is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC IN-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC IN-1 can be used in the research of cholestatic liver injury.

Frenlosirsen sodium is an antisense oligonucleotide targeted to IRF4. It is used for study of relapsed/refractory multiple myeloma (RRMM).

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.

Farabursen sodium (RGLS8429 sodium; RG1015 sodium) is a miR-17 inhibitor. Farabursen sodium inhibits the function of the miR-17 family, relieves the inhibitory effect on miR-17 target genes including PKD1 and PKD2, and increases the level of PC1/2. Farabursen sodium slows the growth of renal cysts, reduces the ratio of kidney weight to body weight, and decreases the cyst index and proliferation index. Farabursen sodium is applicable to research related to autosomal dominant polycystic kidney disease.

FAK activator-1 is a FAK activator and mucosal healing inducer.FAK activator-1 increases FAK phosphorylation at Tyr-397, promoting FAK activation.FAK activator-1 promotes mucosal healing.FAK activator-1 can be used for the research of nsaid-associated gastrointestinal mucosal injury.

FABP4/5-IN-6 is an orally active, potent FABP4/5 inhibitor (Ki = 0.41/2.53 μM), showing low selectivity over FABP3 (Ki = 59.72 μM). FABP4/5-IN-6 inhibits the secretion of MCP-1 and IL-6 in Lipopolysaccharides (LPS)-induced THP-1 macrophage. FABP4/5-IN-6 exhibits significant anti-inflammatory effects and attenuates LPS-induced liver injury. FABP4/5-IN-6 has low hERG inhibition (LD50 > 2000 mg/kg). FABP4/5-IN-6 can be used for the study of Inflammation-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.

ERX-208 is an anticancer agent that induces endoplasmic reticulum stress by targeting lysosomal acid lipase A (LIPA), ultimately leading to cancer cell apoptosis. ERX-208 can be used in ovarian cancer research.

ERG-IN-4 (Compound 12) is an orally active, selective ERG inhibitor with an IC50 of 5.2 μM for hERG. ERG-IN-4 activates PXR. ERG-IN-4 exhibits anticancer activity against MTAP-deleted non-small cell lung cancer.

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.

EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.

EGFR-IN-77 (Compound 4a) is a selective EGFRT790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 functionally inhibits the kinase activities of EGFRT790M/L858R, EGFRL858R and wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer cells. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer.