Cancer Immunotherapy

Sapindoside B is a substance with hepatoprotective activity, and also acts as a cytochrome P-450 (cytochrome P-450) inhibitor, antibacterial agent and membrane-disrupting agent. Sapindoside B reversibly inhibits the content of cytochrome P-450 in liver microsomes, suppresses the phenobarbital-induced increase in enzyme content, reduces the production of active metabolites mediated by cytochrome P-450, and alleviates hepatotoxic injury. Sapindoside B binds to Cutibacterium acnes lipase, reduces lipase activity, inhibits biofilm formation, and decreases bacterial adhesion. Sapindoside B exhibits cytotoxicity against human cancer, liver cancer, leukemia and glioblastoma cells. Sapindoside B inhibits mycelial growth of phytopathogenic fungal strains, possesses antibacterial activity against dermatophytes, and also has hemolytic/membrane-lytic activity. Sapindoside B can be used in research related to liver injury, Cutibacterium acnes biofilm-associated infections, gastric cancer, carcinoma, promyelocytic leukemia, glioblastoma, apple scab and grape gray mold.

Octaethylporphyrin is a porphyrin derivative. Octaethylporphyrin is a photodynamic therapy (PDT) agent.

SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway.

SYS6010 is an antibody-drug conjugate (ADC) targeting epidermal growth factor receptor (EGFR), which is formed by conjugating the anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) with the topoisomerase I inhibitor JS-1 (HY-178217) via a cleavable tetrapeptide linker. SYS6010 can be used in the research of advanced solid tumors such as non-small cell lung cancer.

Datopotamab deruxtecan (DS-1062) is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 K_d of 0.74 nmol/L. Datopotamab deruxtecan consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer.

FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC₅₀ value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS.

Anticancer agent 198 (compound 18b) is a potent anticancer agent and potential WRN protein inhibitor. Anticancer agent 198 was significantly toxic to K562 cells and WRN-overexpressing PC3 cells.

Peretinoin (Standard) is the analytical standard of Peretinoin. This product is intended for research and analytical applications. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1[1]. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM[3].

Quercetin-¹³C₃ is the ¹³C-labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Zoratolimod is a component of the AOC reagent Mozistobart zoratolimod (HY-177568), consisting of a TLR9 agonist and a linker Fmoc-N-PEG24-acid (HY-42360). Zoratolimod can be used to synthesize antibody oligonucleotide conjugates (AOC) such as Mozistobart zoratolimod, which is used in cancer immunology research.

Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach.

Tizetatug rezetecan (SHR-A1921) is an Antibody-drug Conjugate (ADC) composed of antibody Tizetatug (HY-P991032) and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (HY-148668). Tizetatug rezetecan can be used for the research of cancer.

Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC₅₀ values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity.

Bafilomycin A1 (Standard) is the analytical standard of Bafilomycin A1 (HY-100558). This product is intended for research and analytical applications. Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H⁺-ATPase (V-ATPase) with IC₅₀ values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.

Ertapenem (MK-0826) is a broad spectrum and long acting β-lactam antibiotic. Ertapenem has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract.

ARG1-IN-1 (Compound 3) is an orally active arginase inhibitor with an IC₅₀ value of 29 nM. ARG1-IN-1 can inhibit serum arginase activity and increase arginine levels in mouse tumor models. ARG1-IN-1 is applicable for tumor research.

cis a chimeric antigen receptor mRNA targeting CD22. When delivered via CD8-targeted LNP, CD22 CAR mRNA inhibits tumor growth in Nalm6 tumor-bearing mouse models. CD22 CAR mRNA can be used for research on hematologic malignancies.

TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC₅₀ of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

TQB2102 is a bispecific epitope antibody-drug conjugate targeting HER2, composed of the antibody Rolditamig (HY-P992130) and the toxin molecule Deruxtecan-d₂ (HY-13631ES3). TQB2102 binds to the ECD2 and ECD4 domains of HER2, promotes its own internalization by HER2-expressing cells, and delivers deuterated DXd payload to inhibit topoisomerase I. TQB2102 induces antibody-dependent cellular cytotoxicity, DNA damage, bystander killing activity, and inhibits cancer cell proliferation. TQB2102 can be used in research related to various cancers including metastatic breast cancer, colorectal cancer, and gastric/gastroesophageal junction adenocarcinoma.

RIDR-PI-103 is a reactive oxygen species (ROS)-induced agent release proagent with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103). Doxorubicin and RIDR-PI-103 shows a synergistic effect in MDA-MB-361 and MDA-MB-231 cells to inhibit cancer cell proliferation.