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-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma.

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-IN-8 is a selective inhibitor targeting HDAC1, HDAC2 and HDAC3, with IC50 values of 3.52 nM for HDAC1, 15.14 nM for HDAC2 and 0.38 nM for HDAC3. HDAC3-IN-8 shows high selectivity for HDAC3 and exerts its effect by inhibiting histone deacetylase activity. HDAC3-IN-8 can be used to construct HDAC3-targeted PROTAC degrader and is suitable for the research of acute myeloid leukemia (AML).

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.

HDAC1/3-IN-1 is a selective HDAC1/3 inhibitor, with IC50 values of 256 nM and 340.3 nM against HDAC1 and HDAC3, respectively. HDAC1/3-IN-1 increases the SubG1 cell population and promotes apoptosis of glioma cells and glioblastoma stem cells. HDAC1/3-IN-1 can be used in studies related to glioblastoma.

HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury.

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.

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-8 is a pyrazolopyridine derivative and selective HCN2 inhibitor. HCN2 modulator-8 can be used for the research of pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.

HCN2 modulator-6 is a HCN2 ion channel inhibitor has an IC50 of 7 nM. HCN2 modulator-6 inhibits HCN2 ion channel activity. HCN2 modulator-6 can be used for the research of pain, inflammatory pain, neuropathic pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.

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.

HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma.

HBV-IN-56 is an orally active HBsAg production inhibitor. HBV-IN-56 inhibits HBsAg production both in vitro and in vivo. HBV-IN-56 can be used for the research of chronic hepatitis B virus infection.

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.

HAT-IN-10 (Compound 12a) is an anti-human African trypanosomiasis (HAT) agent, with an EC50 value of 0.23 μM for T. brucei. HAT-IN-10 can be used for research on HAT.

Hancockiamide B (Compound 2) is a piperazine alkaloid. Hancockiamide B is isolated from the fungus Aspergillus hancockii.

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.

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.

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.

GuaB-IN-2 (Compound 54) is a GuaB inhibitor, with an IC50 of 0.2 nM for M. tuberculosis GuaB. GuaB-IN-2 can be used in the research of bacterial infections and tuberculosis.

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.

GSPT2 degrader-1 (compound 619) is a selective molecular glue GSPT2 degrader targeting GSPT2. GSPT2 degrader-1 contains Thalidomide and the linker of MDEG-541. GSPT2 degrader-1 induces the degradation, but not GSPT1 or myelocytomatosis oncogene (MYC). GSPT2 degrader-1 can be used for research of gastrointestinal cancer.

GSPT1 degrader-16 (Compound Lib-B-18J) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-16 shows inhibitory effect to RS4;11, Molt4, and MM.1S cells with IC50 values of 0.002, 0.26 and 0.37 μM. GSPT1 degrader-16 can be used for the research of cancer, such as acute lymphoblastic leukemi.