ICI 198615 is a lipoxygenase inhibitor. ICI 198615 inhibits the activity of lipoxygenases involved in eicosanoid metabolism. ICI 198615 attenuates the early phase of bronchoconstriction induced by ET-1.

ICI 185282 is a potent, selective, orally active thromboxane A2 (TXA₂) receptor antagonist. ICI 185282 causes dose-dependent inhibition of U-46619-induced platelet aggregation ex-vivo in guinea-pig. ICI 185,282 inhibits bronchospasm induced by U-46619, PGD2, PGF2α, arachidonic acid, LTD4 and PAF in vivo. ICI 185282 can be used for bronchial asthma research.

ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma.

IC-87361 is a DNA-dependent protein kinase (DNA-PKcs) inhibitor and radiosensitizer. IC-87361 inhibits the catalytic activity of DNA-PKcs and blocks non-homologous end joining (NHEJ) DNA double-strand break repair. IC-87361 can be used for the research of lung cancer and melanoma.

Ibopamine (SB 7505) hydrochloride is an orally active dopamine derivative. Ibopamine hydrochloride exerts agonistic effects on α, β adrenergic receptors and dopaminergic receptors. Ibopamine hydrochloride can be hydrolyzed to produce the active metabolite Epinine. Ibopamine hydrochloride possesses positive inotropic and vasodilatory effects, which can improve hemodynamics and renal function in heart failure models. Ibopamine hydrochloride has good safety profile and can be used in the research of diseases such as congestive heart failure.

IAXO-101 iodide is a TLR4/CD14 blocker. IAXO-101 iodide can inhibit the innate immune pathway of CD14. IAXO-101 iodide is capable of improving the recording performance of intracortical microelectrodes in mice. IAXO-101 iodide can also partially alleviate fetal growth restriction, placental vascular damage, and reduce the level of the inflammatory factor TNF-α in pregnant mice infected with malaria. IAXO-101 iodide can be used in the research of gestational malaria and inflammatory diseases.

IACS-56676 is a selective NRASG12D inhibitor with a target Kd of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity over wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used for research on melanoma, hematologic malignancies and thyroid cancer.

Hydrouracil-(4-Br-2,6-difluorobenzene) is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Hydrouracil-(4-Br-2,6-difluorobenzene) can be linked to a target protein ligand via a linker to form a PROTAC.

Hydrotecan-NH-L-Ala-L-Val-L-Gln(CO-C5-succinimide)-D-glucitol (Example 9) is a conjugate of the ADC toxic molecule and the linker, where the toxic molecule part is Hydrotecan, and the linker part is Mc-Glu(D-Glucamine)-val-ala .

H-Tyr-AMC is a fluorogenic substrate for tyrosine aminopeptidases. H-Tyr-AMC is an inhibitor of tobacco and potato hydroxycinnamoyl-CoA:tyramine N-(hydroxycinnamoyl)transferase (THT) with Ki values of 0.72 μM (tobacco) and 0.42 μM (potato).

Hsp90-IN-47 (Compound C15) is a Hsp90 inhibitor and antifungal agent, with an IC50 of 0.014 μM against Hsp90α. When combined with Fluconazole, Hsp90-IN-47 exerts significant synergistic antifungal effects against fluconazole-resistant Candida albicans 0304103. Hsp90-IN-47 exhibits antitumor activity against acute myeloid leukemia and non-small cell lung cancer.

Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer.

Hsp90-IN-44 (compound 16) is a Hsp90 inhibitor with an IC50 of 9.8 µM. Hsp90-IN-44 can be used for cancer research.

Hsp90-IN-43 (Compound 12) is a Hsp90-TPR2A interaction inhibitor with an IC50 of 360 nM and a Kd of 928 nM. Hsp90-IN-43 effectively inhibits the proliferation of BT474 cells. Hsp90-IN-43 can be used for the study of breast cancer.

HSP90-IN-28 (compound 12 h) is a potent and selective Hsp90 inhibitor with an IC50 of 0.46 μM for Hsp90α. HSP90-IN-28 exhibits ~48 fold selectivity versus other Hsp90β (IC50 = 22.28 μM).

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.

HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal 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.

HO 221 is an orally active benzoylphenylurea derivative with antitumor activity. HO 221 can inhibit the activity of mammalian DNA polymerase alpha. HO 221 can induce G1 phase arrest. HO 221 can be used for the research of cancer, such as leukemia.

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.

HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. HK2-IN-3 reduces glucose uptake and downregulated GLUT1/GLUT4 in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy and apoptosis. HK2-IN-3 suppresses tumor growth and angiogenesis in OSCC xenograft mouse models. HK2-IN-3 can be used for OSCC research.

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-1-IN-88 (compound 20a) is a potent HIV‑1 protease inhibitor (IC50 = 10 pM) with an antiviral EC50 of 10.4 nM. HIV-1-IN-88 exhibits potency against the multidrug-resistant variants HIV-1Muta and HIV-1I50V with EC50 values of 30.0 and 34.3 nM, respectively. HIV-1-IN-88 can be used for HIV 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.

HIV RT-IN-1 is an inhibitor of HIV integrase and HIV reverse transcriptase-associated ribonuclease H. HIV RT-IN-1 is applicable to research related to 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.