Cancer Immunotherapy

FEN1-IN-2 (compound 20) is a flap endonuclease 1 (FEN1) inhibitor, with IC50 values of 3 nM and 226 nM for FEN1 and XPG, respectively.

Tenuazonic acid is a nonhost-selective mycotoxin belonging to the tetramic acids family. Tenuazonic acid inhibits protein biosynthesis on ribosomes by suppressing the release of new protein. Tenuazonic acid is acutely toxic, and oral LD₅₀ is set between 81-186 mg/kg in rats and mice. Tenuazonic acid blocks electron transport beyond the primary quinone receptor (QA) by interacting with the D1 protein and is a photosystem II (PSII) inhibitor. In addition, Tenuazonic acid has antiviral effects on measles virus, enterovirus, respiratory virus and so on. Tenuazonic acid has an inhibitory effect on skin cancer.

MC-Val-Cit-PAB-Ispinesib (Compound 509) is a drug-linker conjugate for ADC, consisting of a cleavable ADC linker and Eg5 inhibitor. MC-Val-Cit-PAB-Ispinesib can be used for the synthesis of antibody-drug conjugates (ADCs).

Chaetoglobosin A is a secondary metabolite and nematicide. Chaetoglobosin A is produced by Penicillium aquamarinium. Chaetoglobosin A targets Filamentous actin in cells, thereby inducing cell cycle arrest, and inhibiting membrane ruffle formation and cell migration. Chaetoglobosin A preferentially induces Apoptosis in chronic lymphocytic leukemia cells. Chaetoglobosin A induces dose- and time-dependent death in J2 larvae of the southern root-knot nematode (Meloidogyne incognita). Chaetoglobosin A can be used in studies related to root-knot nematode disease and chronic lymphocytic leukemia.

Quinoclamine, a naphthoquinone derivative, is a NF-κB inhibitor. Quinoclamine exhibits anti-cancer activity.

L-Histidine-d₅ hydrochloride hydrate is the deuterium labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable.

Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human TFA induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human TFA also induces apoptosis. Angiotensin II human TFA induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.

Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation.

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.

FAP-IN-2 is an isonitrile-containing fibroblast activation protein (FAP) inhibitor. FAP-IN-2 can be labeled with technetium-99m (^99mTc) for targeted tumor SPECT imaging.

MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) is a reversible proteasome inhibitor. MG-262 down-regulates VEGF receptor Flt-1. MG-262 inhibits cell growth and induces apoptosis in malignant cells. MG-262 induces reactive oxygen species (ROS). MG-262 can be used for anti-cancer study.

Mal-C2-Gly3-EDA-PNU-159682, a agent-linker conjugate for ADC, consists a cleavable ADC linker Mal-C2-Gly3-EDA and a potent ADC cytotoxin PNU-159682.

Crocin III is a crocin isolated from Crocus sativus L. Crocins inhibit the growth of tumor cells and exhibit anti-inflammatory activity.

CVRARTR is a programmed cell death ligand-1 (PD-L1) antagonist with a K_D of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and T cell proliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model. CVRARTR can be used in melanoma research.

BRITE-338733 is an inhibitor of E. coli RecA ATPase activity (IC₅₀: 4.7 μM). BRITE-338733 also inhibits the ATP hydrolysis activity of RSC chromatin remodeling enzyme by binding to its ATP-binding pocket and DNA (IC₅₀: 0.316 μM). BRITE-338733 exhibits cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. BRITE-338733 can be used in studies on antibacterial adjuvants and anticancer research.

DiR (solution) is a long-chain carbocyanine dye. Carbocyanine dyes are widely used as Di to label cells, organelles, liposomes, viruses and lipoproteins.
Solvent and concentration: DMSO: 5 mM

5-Methoxyindole is an L-tryptophan metabolite with antifungal activity, and also serves as a pharmaceutical intermediate. Metabolites of 5-Methoxyindole exhibit COX-2 inhibitory, anti-inflammatory and anti-tumor activities. 5-Methoxyindole induces morphological distortion of hyphae and conidia, ROS accumulation, apoptosis and cell death in Gaeumannomyces graminis. 5-Methoxyindole can be used in studies related to fungal infections and organic synthesis.

Propargyl-PEG4-NHS ester is a nonclaevable 4-unit PEG linker for antibody-agent-conjugation (ADC). Propargyl-PEG4-NHS ester is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Moracin O is a 2-arylbenzofuran isolated from the Morus alba Linn. . Moracin O exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects.

S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-allylmercaptocysteine achieves its anti-cancer effect through a variety of pathways such as inducing the apoptosis of cancer cells through the TGF-β signaling pathway, or reducing the NF-κB activity and up-regulating Nrf2 to achieve the effects of anti-inflammation and anti-oxidation.