Cancer Immunotherapy

Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research.

BRD7586 is a potent and selective Streptococcus pyogenes Cas9 (SpCas9) inhibitor. BRD7586 specifically engages SpCas9 but not Cas12a in cells and enhances SpCas9 specificity at multiple loci. BRD7586 inhibits SpCas9 at multiple genomic loci irrespective of the mode of SpCas9 delivery.

AZ'9567 is an orally active MAT2a inhibitor with a pIC₅₀ of 9.1. AZ'9567 binds to MAT2a allosterically, reduces the synthesis of SAM, decreases SDMA levels, and exerts antiproliferative effects on MTAP-knockout cells. AZ'9567 depletes SAM, causes methionine accumulation in plasma and tissues, triggers adaptive disorders in one-carbon metabolism, transsulfuration metabolism and lipid metabolism, and induces oxidative stress, hepatic steatosis and lipid homeostasis imbalance. AZ'9567 can be used in studies related to MTAP-deficient/deleted cancers.

Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.

IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC₅₀ = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC₅₀ = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation.

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

Volrustomig (MEDI-5752) is a human IgG1 κ monoclonal antibody targeting CTLA4/PD1. The isotype control for Volrustomig is Human IgG1 kappa, Isotype Control (HY-P99001). Volrustomig anchors to the surface of T cells by binding PD-1, induces PD-1 internalization and degradation, and preferentially inhibits CTLA-4 on activated PD-1⁺ T cells. Volrustomig binds to tumor-infiltrating lymphocytes and a subset of PD-1⁺ B cells, enhances T cell function and IFNγ secretion. Volrustomig reduces the activation of non-tumor-infiltrating lymphocytes and exhibits manageable toxicity. Volrustomig can be used in research on various cancers, such as non-small cell lung cancer, gastric cancer, hepatobiliary cancer, and cervical cancer.

SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)^Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF^Met30.

Mc-Gly-Gly-Phe-Gly-PAB-OH (Mc-GGFG-PAB-OH) is a cleavable ADC linker used for antibody-drug conjugates (ADCs).

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

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.

3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.

Amino-PEG8-Boc is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-PEG8-Boc is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

NGM-120 is a fully humanized IgG1 monoclonal antibody targeting GFRAL, which functions by blocking the GDF15-GFRAL axis. NGM-120 reduces serum GDF15 levels, increases body weight, expands central memory and proliferative CD8⁺ T cell populations, and decreases immunosuppressive and naive regulatory T cell populations. NGM-120 can be used for research on advanced prostate cancer.

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.

ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K⁺ channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation. Ex/Em=587/615 nm.
Solvent and concentration: DMSO: 1 mM

Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.

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.

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.

L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a K_D of 1.3±0.3 µM, and a K_inact of 0.15±0.03 min^-1.