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.

HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin. HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer.

Homidium chloride is a potent antiparasitic agent exhibiting activity against Trypanosoma rhodesiense and Trypanosoma congolense. Homidium chloride can reduce parasitaemia in murine models of infection. Homidium chloride can be used for trypanosomiasis research.

HMN-1180 is a selective, competitive neuronal nitric oxide synthase (nNOS) inhibitor with a Ki value of 5.4 μM against rat nNOS. HMN-1180 exerts no significant effect on endothelial nitric oxide synthase (eNOS) or inducible nitric oxide synthase (iNOS). HMN-1180 inhibits nitric oxide production in neuroblastoma cells. HMN-1180 can be used for the study of nNOS-related neuronal functional physiology.

HKC54 is a selective TRPV2 antagonist with an IC50 of 0.4 μM. HKC54 binds directly to TRPV2 and inhibits TRPV2-mediated calcium influx. HKC54 inhibits glioblastoma cell migration in vitro and breast cancer metastasis in vivo. HKC54 can be used for the research of breast cancer lung metastasis.

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.

HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2.

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.

Hexoprenaline sulfate is an orally active and selective β-adrenergic receptor agonist. Hexoprenaline sulfate can dilate the bronchi. Hexoprenaline sulfate can activate adenylate cyclase and increases 14C-Aminopyrine uptake. Hexoprenaline sulfate exhibits anti-infection and anti-inflammmation effect. Hexoprenaline sulfate can increase placental weight and blood flow. Hexoprenaline sulfate can be used for the researches of inflammation, immunology, infection, endocrinology and neurological disease, such as asthma, chronic bronchitis, sepsis and intoxication of organophosphorus compounds.

Hexane-2,5-dione (2,5-HD) is a cytotoxic agent. Hexane-2,5-dione causes an accumulation of neurofilaments within axons in rats that may lead to their degeneration. Hexane-2,5-dione is promising for research of neurodegenerative diseases (e.g., Alzheimer's, Parkinson's).

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.

HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer.

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-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research.

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.

HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging.

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.

HDAC1-IN-10 (Compound 2b) is a potent, selective and orally active HDAC1/2 inhibitor with IC50 values of 6 and 190 nM. HDAC1-IN-10 shows IC50 > 50 μM for HDAC3-8. HDAC1-IN-10 can inhibit tumor growth in HCT-116 colon xenograft nude mice model. HDAC1-IN-10 can be used for research of colon cancer.

HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, and Kd values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease.

HCV NS5B polymerase-IN-4 is a HCV NS5B polymerase inhibitor with an IC50 of 4.2 μM. HCV NS5B polymerase-IN-4 binds to the active site of this enzyme. HCV NS5B polymerase-IN-4 can be used in studies related to hepatitis C virus (HCV) infection.