Cancer Immunotherapy

Leelamine hydrochloride is an orally active weakly basic amine that inhibits NPC1 and the androgen receptor AR-V7, and acts as a cannabinoid receptor agonist. Leelamine hydrochloride also functions as a lysosome affinity agent that blocks endocytosis, disrupts autophagic flux and cholesterol transport, thereby altering the RTK-AKT/STAT/MAPK signaling cascade. Leelamine hydrochloride induces cancer cell death and autophagosome accumulation, and can be used in research related to melanoma, castration-resistant prostate cancer and breast cancer.

m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugate (ADC) for Trastuzumab (HY-P9907). m-PEG4-Br is placed distally from the monomethyl auristatin E (MMAE) payload to yield an ADC with altered hydrophilicity, antigen binding, and in vitro potency. m-PEG4-Br also can be used as a PROTAC linker that can be used in the synthesis of PROTACs.

PY159 is a humanized antibody targeting TREM1/CD354. PY159 reprograms immunosuppressive intratumoral myeloid cells towards an inflammatory, anti-tumor phenotype, promotes anti-tumor immune responses, upregulates monocyte activation markers, and induces proinflammatory cytokines. PY159 can be used for the research of platinum-resistant ovarian cancer, advanced solid tumors, and advanced refractory solid tumors.

L-Ascorbic acid-d₂ is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla

Psammaplysene A, a brominated tyrosine derivative, can promote the nuclear localization of FOXO1, leading to cell cycle arrest and apoptosis, and can be used in cancer research.

PROTAC JAK1 degrader 1 is a JAK1 PROTAC degrader with a DC₅₀ of 214 nM and an IC₅₀ of 5.2 nM. PROTAC JAK1 degrader 1 inhibits the downstream JAK-STAT signaling pathway by degrading JAK1. PROTAC JAK1 degrader 1 exhibits antiproliferative activity in cells. PROTAC JAK1 degrader 1 can be used for research on leukemia.

Anti-Mouse NKG2D/CD314 Antibody (CX5) is a rat-derived IgG1 κ type antibody inhibitor, targeting to mouse NKG2D/CD314. Anti-Mouse NKG2D/CD314 Antibody (CX5) reduces cytotoxicity of natural killer cells. Anti-Mouse NKG2D/CD314 Antibody (CX5) can be used for the researches of cancer, infection, inflammation, immunology and metabolic disease, such as colitis and diabetes.

Calphostin C is a highly selective PKC inhibitor (IC₅₀=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications.

1-Boc-azetidine-3-carboxylic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Boc-azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[2]

Loliolide (Loliolid) is a β-carotene metabolite. Loliolide reduces caspase 3, 8, 9 expression, enhances PI3K, AKT, SIRT1, inhibits ROS, apoptosis, and blocks NF-κB p65 nuclear translocation. Loliolide protects mitochondria, reduces oxidative stress, and increases cell viability in neuroblastoma cells. Loliolide can be used for the research of UV-induced skin damage and Parkinson’s disease.

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8⁺ T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer.

OTUB2-IN-1, a specific inhibitor of OTUB2 (K_D: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .

Boc-NH-PEG6-CH2CH2COOH is a cleavable ADC linker used as a linker for antibody-drug conjugates (ADC). Boc-NH-PEG6-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.

Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with antitumor activity.

GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC₅₀=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

PBD dimer-2 (compound 2c) is a C8-linked pyrrolobenzodiazepine dimer. PBD dimer-2 can span an extra base pair and cross-link the 5′-Pu-GA(T/A)TC-Py sequence. PBD dimer-2 can be used as a payload for antibody–agent conjugates (ADCs), and it can be used for the research of cancer.

DEL-S1 is a SLIT2 binder. DEL-S1 significantly inhibits the formation of the SLIT2/ROBO1 complex by inducing conformational rearrangement, and further suppresses its function, with an IC₅₀ of 68.8 μM. DEL-S1 can be used in studies of neurodevelopment, immunomodulation, and cancers such as glioblastoma.

Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

N-Nitrosomorpholine is a photosensitive nitrosamine that is carcinogenic and can be used to construct animal cancer models.