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.

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.

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.

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-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.

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).