immunogenic

PEG300 (Polyethylene glycol 300) is a polymer formed from repeating units of ethylene glycol that is water soluble, low immunogenicity, and biocompatible. PEG300 is a neutral polymer with a molecular weight of 300.

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

GW280264X (Carbamic acid) is an inhibitor of ADAM17 .

Lipopolysaccharides (LPS), derived from Escherichia coli O55:B5, are essential components of the outer membrane of Gram-negative bacteria. Composed of lipid A, a core oligosaccharide, and an O-specific polysaccharide, LPS exhibits strong immunogenicity. It activates immune cells via the TLR4 receptor, induces chemotactic cell migration and cytokine secretion, and helps maintain the integrity of the bacterial outer membrane, protecting against bile salts and lipid-based antibiotics. LPS is commonly used to establish inflammatory models, including arthritis, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome (ARDS), and gastrointestinal disease models.

HPV16 E7 (86-93) acetate is a derived peptide of human leukocyte antigen A2.1 restricted HPV16 E7 with immunogenic property in cervical carcinomas.

(5Z,2E)-CU-3 is a potent and highly selective inhibitor of the DGKα isozyme with an IC50 value of 0.6 μM, competing with ATP and exhibiting a Km value of 0.48 mM. It specifically targets the catalytic region of DGKα without affecting the regulatory region and has demonstrated antitumor and immunogenic effects by promoting cancer cell apoptosis and T cell activation.

CP-20961 is an effective synthetic non-immunogenic adjuvant that can be used to induce acute and chronic arthritis models.

ERK-MYD88 Interaction Inhibitor 1, an agent that disrupts the interaction between ERK and MYD88, has demonstrated the ability to trigger an HRI-mediated integrated stress response (ISR) that specifically promotes immunogenic cell apoptosis (apoptosis) in cancer cells. Additionally, in models using Lewis lung cancer mice, this compound has been shown to stimulate anti-tumor T cell responses, thereby exhibiting significant anti-tumor activity.

Sulfamethoxazole-NO (SMX-NO) is a SMX-NO derivative that is a major immunogen for sulfonamide hypersensitivity reactions, is cytotoxic, and is immunogenic in rodents.

Photosensitizer-6 (Compound 4) is a metal ion complex that inhibits TrxR. It induces apoptosis in 4T1 cells, targeting cancer cells and eliminating tumors through chemophototherapy and immunogenic cell death under illumination. Additionally, Photosensitizer-6 can be utilized for tumor imaging.

ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.

ROS-ERS inducer 2 (Complex 3f) promotes the generation of intracellular ROS, affects mitochondrial function, facilitates the release of damage-associated molecular patterns (DAMPs), induces immunogenic cell death (ICD), and activates endoplasmic reticulum stress (ERS). It plays a significant role in anti-hepatocellular carcinoma research.

IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug that suppresses IDO expression. It induces apoptosis, reduces mitochondrial membrane potential, and inhibits tumor cell migration and invasion. Additionally, IDOi-Pt(IV) prodrug-1 triggers reactive oxygen species-mediated endoplasmic reticulum stress and the secretion of damage-associated molecular patterns (DAMPs), leading to immunogenic cell death (ICD). Compared to cisplatin, IDOi-Pt(IV) prodrug-1 exhibits relatively high efficiency and low toxicity in its antitumor activity.

ICD inducer-1 (Compound Re1) is an effective inducer of immunogenic cell death (ICD), targeting the endoplasmic reticulum (ER) and subsequently inhibiting ER phagocytosis. It shows promise for cancer research.

TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.

Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.

Tubulin polymerization/V-ATPase-IN-1 (compound F10) is an inhibitor of tubulin polymerization and V-ATPase. It exhibits potent antiproliferative activity against four types of human cancer cells by inhibiting both tubulin and V-ATPase. The compound also induces apoptosis and immunogenic cell death while suppressing tumor growth in the RM-1 allograft model with enhanced T lymphocyte infiltration.

Telomeric G4s ligand 1 is a telomere G-quadruplex ligand that stabilizes telomeric G4 structures and induces the formation of R-loops, leading to DNA damage responses. It prompts apoptosis in tumor cells and triggers immunogenic cell death (ICD).

a15:0-i15:0 PE is a dia-cyl phosphatidylethanolamine with two branched chains. It functions as an atypical TLR2-TLR1 heterodimer agonist and is immunogenic. This compound activates T cell and dendritic cell (DC) signaling, exhibiting anti-inflammatory properties. Additionally, a15:0-i15:0 PE induces the production of TNFα and IL-6. It is a major component of the A. muciniphila lipid membrane, constituting approximately 50%.

Anticanceragent 292 (Compound P4) is a photosensitizer targeting melanoma. It exhibits good biocompatibility in the absence of light and, when exposed to light, induces apoptosis and partial necrosis of B16-F10 cells by disrupting lysosomal membranes. Furthermore, Anticanceragent 292 not only directly kills tumor cells through generated ROS but also induces immunogenic cell death (ICD), leading to antitumor immune responses. This compound is applicable for research in photodynamic therapy for melanoma.

STAT3-IN-51 is a STAT3 inhibitor that binds directly to the SH2 domain of STAT3. This compound induces apoptosis, ferroptosis, and immunogenic cell death (ICD), enhancing antitumor immunity. It suppresses STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling, while prompting reactive oxygen species (ROS) generation, decreasing Bcl-2 expression, disrupting mitochondrial functions, inhibiting GPX4 activity, and promoting lipid peroxidation. STAT3-IN-51 is applicable in research on colorectal cancer, breast adenocarcinoma, non-small cell lung cancer (NSCLC), and cisplatin-resistant lung adenocarcinoma.

Pt(II)-NHC Complex 2C (Platinum(II)-N-Heterocyclic carbene complex 2C) (Compound 2C) is an N-heterocyclic carbene-based platinum (II) complex. This compound acts as an immunogenic cell death (ICD) inducer in liver cancer cells, triggering endoplasmic reticulum stress (ERS) and ROS production, which ultimately leads to the release of damage-associated molecular patterns (DAMPs). Furthermore, it arrests the cell cycle in the S phase and significantly induces apoptosis. In mouse models, Pt(II)-NHC Complex 2C has demonstrated anticancer potential against liver cancer and activated immune cells in liver injury models.

FGFR-IN-25 (Compound 19E) is an FGFR inhibitor with IC50 values of 1.30 nM for FGFR1 and 0.85 nM for FGFR2, and also acts as a radiosensitizer. It effectively reduces the phosphorylation levels of FGFR1 and its downstream effectors, pAKT and pERK. FGFR-IN-25 exhibits broad-spectrum antitumor activity against gastric, colorectal, liver, breast, triple-negative breast cancers, and glioblastoma. When combined with radiation therapy, FGFR-IN-25 synergistically activates the ROS-Caspase-3-GSDME pathway, downregulates PD-L1 expression, and induces immunogenic cell death, thereby enhancing the antitumor effects.

Tigilanol tiglate (EBC-46) is a PKC/C1 domain activator. Tigilanol tiglate promotes mitochondrial/endoplasmic reticulum dysfunction, leading to ATP depletion, caspase activation, and gasdermin E cleavage. It induces immunogenic cell death, enhancing the response to immune checkpoint blockade in both target tumours and non-injected tumours, resulting in tumour regression.