IL-17-IN-4 (Compound 3) is an IL-17 inhibitor with an IC50 of less than 0.1 μM. IL-17-IN-4 can be used for the study of inflammatory diseases.

IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM.

IKKε-IN-1 is a IKKε inhibitor. IKKε-IN-1 reduces cell viability, inhibits colony formation and cell migration. IKKε-IN-1 induces autophagy (Autophagy) in cancer cells. IKKε-IN-1 can be used in the research of cancers including colorectal cancer, hepatocellular carcinoma, bladder cancer, breast cancer, lung cancer, and cervical cancer.

IKKβ-IN-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer.

IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.

Ikarisoside B is a potent and selective Organic cation transporter 1 (OCT1) inhibitor with an IC50 of 11.18 μM. Ikarisoside B shows selectivity over OCT2 (IC50 = 56.54 μM). Ikarisoside B can be used for the research of metabolic disease.

IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers.

IHCH-3185 is an orally active class I HDAC inhibitor (HDAC1 IC50 =102.9 nM) and A2AR antagonist (A2AR Ki =7.6 nM). IHCH-3185 reverses immune gene silencing by inducing histone acetylation and blocks the adenosine signaling pathway to relieve T-cell suppression. IHCH-3185 exhibits antiproliferative activity, induces cell cycle arrest, and significantly improves the tumor microenvironment. IHCH-3185 reduces the proportion of regulatory T cells, increases the CD8+/Treg ratio, and upregulates the expression of key factors such as H2-K1, Cxcl9 and Cxcl10. IHCH-3185 shows significant antitumor potential in CT26 and MC38 mouse tumor models and is suitable for related cancer research.

IDO1-IN-32 (Compound 45) is a potent and orally effective IDO1 inhibitor with an IC50 of 10 pM. IDO1-IN-32 exhibits significant anti-proliferative activity against Hela cells. IDO1-IN-32 can significantly inhibit tumor growth in CT26 and LCC transplanted mouse models by activating anti-tumor immunity. IDO1-IN-32 can be used for research on colon cancer and breast cancer.

IDO1-IN-31 (Compound 17g) is an IDO1 agonist with an IC50 of 77 nM. IDO1-IN-31 can be used for the study of neurological diseases and cancers.

IDO1-IN-30 (Compound (R)-100) is a potent and highly selective IDO1 inhibitor. IDO1-IN-30 has an IC50 of 4.8 nM to IDO1 in SKOV3 cells. IDO1-IN-30 does not show significant cytotoxicity at 25 µM in HepG2 cells. IDO1-IN-30 can eliminate inhibition of CYP450 enzymes (such as 3A4, 2C9, 2D6). IDO1-IN-30 can be used for research on cancer and inflammatory conditions.

IDO1/TDO-IN-11 (Compound Y-13) is a dual IDO1 and TDO inhibitor, with an IC50 of 2.87 μM against hIDO1 and an IC50 of 0.08 μM against hTDO. IDO1/TDO-IN-11 inhibits NO production and ROS production. IDO1/TDO-IN-11 alleviates cellular neuroinflammatory damage and ameliorates Parkinson's disease. IDO1/TDO-IN-11 is applicable to research related to Parkinson's disease.

IDH1 ligand 1 (Compound 18) can serve as a negative control for the IDH1 target, with no detectable affinity for wild-type IDH1 and an IC50 >10,000 nM.

ICI-200880 is a potent, selective and reversible human neutrophil elastase (HNE) inhibitor. ICI-200880 is promising for research of inflammatory lung diseases related to neutrophil elastase, such as chronic obstructive pulmonary disease (COPD) and cystic fibrosis (CF).

ICI-170777 is an orally active cardiotonic agent. ICI-170777 enhances cardiac contractility and induces arteriovenous dilation in animal models of congestive heart failure. ICI-170777 can be used in research on cardiovascular and cerebrovascular diseases such as heart failure.

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).