GSPT1 degrader-15 (Compound Lib-B-15O) is a potent and highly selective GSPT1 molecular gel degrader, with a DC50 of 154 nM. GSPT1 degrader-15 has almost no effect on the expression of other proteins. GSPT1 degrader-15 exhibits significant anti-proliferative activity against leukemia cells and lymphoma cells. GSPT1 degrader-15 can be used in leukemia and lymphoma research.

GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC50 of 2 nM and a PLK3 IC50 of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC50: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian cancer.

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

GSK190937 is a type II platelet-derived growth factor receptor alpha (PDGFRA) human kinase inhibitor with antimalarial activity. GSK190937 can inhibit the formation of hemozoin in the malaria parasite, resulting in the accumulation of free hemoglobin within the malaria parasite. GSK190937 shows IC50 values of 0.22, 0.59 and 0.25 μM against P. falciparum NF54, K1 and Dd2 parasite. GSK190937 shows an IC50 of 25 μM for CHO cells. GSK190937 can be used for research of malaria.

GSK 1997132B is a benzimidazole-based PPARγ partial agonist that can cross the blood-brain barrier with a pEC50 value of 8.0. GSK 1997132B has no significant effect on PPARα/δ. GSK 1997132B improves the problem of high blood clearance rate of earlier compounds, avoiding side effects such as weight gain and edema. GSK 1997132B can be used for research on Alzheimer's disease.

GSK 124576A (compound 8) is a Mycobacterium tuberculosis cytochrome bc1 complex inhibitor and member of the 2-(quinolin-4-yloxy)acetamide class. GSK 124576A can be used for the research of tuberculosis.

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.

GRP75-IN-1 (Compound 33) is an anti-endometrial cancer (EC) agent. GRP75-IN-1 induces apoptosis in endometrial cancer cells. GRP75-IN-1 hydrochloride reduces mitochondrial Ca2+ levels by targeting GRP75 and disrupting its interaction with IP3R. GRP75-IN-1 inhibits tumor growth in human endometrial cancer xenograft animal models. GRP75-IN-1 can be used for research in endometrial cancer.

GRM1 modulator-1 is a GRM1 modulator.

GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy.

GRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research.

GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasive and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA), and consequently inhibiting ATX-LPA axis-related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 (IC50=31.42 nM, Ki=12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus.

Graviquinone is a Chk1 inhibitor. Graviquinone exhibits potent cytotoxicity against various cancer cell lines. Graviquinone possesses the characteristics of bypassing ABCB1-mediated multidrug resistance, selectively damaging cancer cell DNA, and regulating the DNA damage response. Graviquinone can also enhance cytotoxicity by increasing ROS levels in cancer cells. Graviquinone can be used for cancer 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).

GPX4-IN-1 is a potent GPX4 inhibitor. GPX4 shows antiproliferative activity. GPX4-IN-1 has the potential for the research of cancer.

GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model.

GPR84 antagonist 10 (compound 1) is a potent and orally active GPR84 antagonist. GPR84 antagonist 10 can be used to study GPR84-dependent diseases, such as inflammation-driven pain diseases.

GPR6 inverse agonist 2 (Compound 575) is a selective GPR6 inverse agonist, with IC50 values of < 0.1 μM and 1~30 μM against GPR6 and GPR3, respectively. GPR6 inverse agonist 2 exhibits preliminary cardiac safety, with an IC50 of 21.71 μM for hERG. GPR6 inverse agonist 2 can be used in the research of movement disorders such as Parkinson's disease.

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.

GPR17 agonist 1 is a selective and potent GPR17 agonist with an EC50 of 35 pM. GPR17 agonist 1 also shows weak activation of P2Y Receptor. GPR17 agonist 1 can be used for the research of neurological disease.

GPR119 agonist 4 is a GPR119 agonist and oral glucose-lowering agent with a human GPR119 EC50 of 42 nM.GPR119 agonist 4 activates GPR119.GPR119 agonist 4 reduces blood glucose area under the curve in an oral glucose tolerance test.GPR119 agonist 4 exhibits improved clearance in liver microsomes.GPR119 agonist 4 can be used for the research of type 2 diabetes mellitus.

GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock.

GP130 (G130) is a psychostimulant agent, exhibiting antagonist activity against central nervous system depressing agents[2.

Gosogliptin hydrochloride is the hydrochloride of Gosogliptin. Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity. Gosogliptin stimulates insulin secretion and improves glucose tolerance.

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.

GNE-140 is an orally active and selective inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC50 values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. GNE-140 attenuates cardiac hypertrophy, alleviates PM2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression, regulates metabolites of glycolysis and the pentose phosphate pathway, reduces glucose uptake, increases ROS, and induces cancer cell apoptosis. GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer.

GMNN modulator-1 is a GMNN modulator.

Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research.