HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors.

CDK6-IN-2 is a CDK6 covalent inhibitor with an IC50 of 0.013 μM. CDK6-IN-2 inhibits the proliferation and migration of triple-negative breast cancer cells, and induces cell cycle arrest and apoptosis. CDK6-IN-2 induces ROS accumulation and mitochondrial damage through cellular metabolic reprogramming. CDK6-IN-2 exhibits anti-tumor activity and can be used for the research of triple-negative breast cancer.

HIV-IN-13 prodrug (Compound 8) is a prodrug of an HIV inhibitor. Without the addition of glutathione (GSH), the HIV-IN-13 prodrug has no antiviral activity, but when 1 mM and 2 mM GSH are added, the EC50 values for HIV-1 are 10 μM and 8.2 μM respectively. HIV-IN-13 prodrug can be used in HIV infection research.

HIV RT-IN-2 is a HIV reverse transcriptase inhibitor with an IC50 value of 1.2 μM for HIV-1 RT RNA-dependent DNA polymerase. HIV RT-IN-2 potently inhibits all three modes of HIV-1 RT-associated RNase H activity (internal, 3'-DNA directed, 5'-RNA directed cleavage) and inhibits HIV-1 replication. HIV RT-IN-2 can be used for the research of HIV-1 infection.

His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer. (Pink: ERRα Target protein ligand; Blue: Ligands for E3 Ligase ligand ; Black: linker).

Histamine glutarimide (XC8) is an orally active anti-asthma agent. Histamine glutarimide blocks the maturation of chemokines (CCL2, CCL7, CCL8, CCL13) and inhibits the migration of eosinophils and the degranulation of mast cells. In asthma models induced by carrageenan and rat ovalbumin, Histamine glutarimide can reduce airway resistance and the count of eosinophils in bronchoalveolar lavage fluid. Histamine glutarimide can be used in asthma research.

H-Ile-Ala-OH (Ile-Ala; L-Isoleucyl-L-alanine) is a linear aliphatic dipeptide and self-reactive cyclization reagent that self-assembles into amorphous films or spherical structures from specific solvents. H-Ile-Ala-OH also serves as a precursor for the synthesis of the cyclic peptide cyclo (L-isoleucyl-L-alanine). H-Ile-Ala-OH undergoes solid-state cyclization when heated above 206 °C, and its initiation temperature is closely related to the size of side-chain substituents.

HI-280 is a human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitor. HI-280 can be used for the research of infection.

HGF-IN-1 ((the compound on the left in the second line of page 77) is a HGF inhibitor. HGF-IN-1 can be used in cancer research.

Herbicide safener-1 (II-Q001) is a crop protection and safety agent. Herbicide safener-1 can protect crops from the damage caused by pesticides (such as herbicides and fungicides).

Herbicidal agent 15 is a uracilpyridine herbicide. Herbicidal agent 15 controls harmful plants and acts on plants, their seeds, and their habitat to manage unwanted vegetation.

Hepoxilin A3 (HXA3) is a neutrophil chemo-attractant, synthesized by activating the PLA2-12-LOX pathway. Hepoxilin A3 can guide neutrophils to cross the epithelial barrier and migrate to the infection site (such as the alveolar cavity). The level of Hepoxilin A3 increases synchronously with neutrophil infiltration in mouse models. Hepoxilin A3 can be used to study inflammatory diseases (such as pneumonia, cystic fibrosis).

HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 inhibits the enzymatic activity of HDAC and exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.

HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.

HDAC6-IN-77 is a highly selective HDAC6 inhibitor with an IC50 of 7.0 nM.HDAC6-IN-77 induces neurite outgrowth.HDAC6-IN-77 exerts neuroprotective activity.HDAC6-IN-77 shows no significant toxicity on dopaminergic cells.HDAC6-IN-77 can be used for the research of Alzheimer's disease.

HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.

HCN2-IN-5 is a HCN2 ion channel inhibitor with an IC50 of 9 nM. HCN2-IN-5 shows weak inhibitory activity for HCN4. HCN2-IN-5 can be used for the research of inflammatory disease and neurological disorders.

HCN2-IN-2 (Compound 35), azaindazole derivative, is a selective HCN2 inhibitor with an IC50 of 145 nM. HCN2-IN-2 inhibits HCN2 channel activity blocks abnormal firing of peripheral nociceptive neurons. HCN2-IN-2 can be used for the research of pain.

HCN2 modulator-5 (S-configuration 39) is a HCN2 ion channel inhibitor. HCN2 modulator-5 inhibits HCN2 ion channel activity. HCN2 modulator-5 can be used for the research of pain, inflammatory pain, neuropathic pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.

GyrB-IN-1 is a DNA gyrase (GyrB) inhibitor. GyrB-IN-1 shows an IC50 of 19.1 μM against Mycobacterium smegmatis GyrB ATPase activity and 21.9 μM against Mycobacterium tuberculosis GyrB DNA supercoiling activity. GyrB-IN-1 exerts antimycobacterial activity and has cytotoxicity. GyrB-IN-1 can be used for the research of tuberculosis.

GW583340 (compound 6) is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW583340 exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW583340 is applicable to research related to head and neck cancer, breast cancer, and gastric cancer.

GW-5823 is a selective CCK-AR agonist with an EC50 of 70 nM. GW-5823 can be studied in research on obesity.

Guraxetan-NH-PEG3-TFP ester (Fig.3) is a chelating agent and linker conjugate that can be used in the synthesis of radiopharmaceuticals.

Guanosine 5'-triphosphate 3'-diphosphate is a guanine nucleotide that participates in RNA synthesis and protein synthesis.

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.

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 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.