Cancer Immunotherapy

Nimorazole (K-1900), a 2-nitroimidazole, is a hypoxic cell-radiation sensitizer. Nimorazole has anti-infective and anti-protozoal against trichomoniasis. Nimorazole has the potential for head and neck cancer.

Gotistobart (ONC-392; BNT 316) is a humanized anti-CTLA-4 antibody with selective regulatory T cell depletion activity in the tumor microenvironment. Gotistobart can be used for the research of cancer, such as non-small cell lung cancer.

CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar K_d value. CC-90002 can be used for the research of hematologic malignancies and solid tumors.

Colesevelam hydrochloride is an orally active bile acid sequestrant, lipid-lowering agent, and glycemic control agent. Colesevelam hydrochloride binds bile acids in the gastrointestinal tract to form nonabsorbable complexes, interrupts enterohepatic recirculation and increases fecal bile acid elimination. Colesevelam hydrochloride modulates FXR, TGR5, and Cyp7a1 activity and triggers cAMP signaling and GLP-1 release. Colesevelam hydrochloride alters hepatic lipid and glucose metabolism, suppresses hepatic glycogenolysis, reduces hepatic triglyceride and cholesterol levels, and increases LDL-C (low-density lipoprotein cholesterol) clearance. Colesevelam hydrochloride can be used for the research of type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC₅₀ of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC₅₀ of 95 nM). TAS-119 has potent antitumor activites.

Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse IL-7Rα/CD127. Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) blocks IL-7 signaling. Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) can be used for the researches of cancer,infection, inflammation, immunology, cardiovascular and metabolic disease, such as abdominal aortic aneurysms, helicobacter felis-induced gastritis and diabetes.

Khasianine is a steroidal glycoalkaloid. Khasianine alleviates psoriasis-like skin inflammation by inhibiting the TNF-α/NF-κB axis. Khasianine can downregulate the RhoA pathway and exhibits potential antimetastatic activity. Khasianine upregulates the expression of TNFR I and TNFR II without inducing apoptotic effects. Khasianine can be used in studies related to psoriasis, pancreatic ductal adenocarcinoma, and liver cancer.

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

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.

TLR7/8 agonist 3 (Compound II) is a potent TLR7 and TLR8 agonist, extracted from patent WO2016057618 (compound of formula (II)).

Hex is an enolase inhibitor and antimalarial agent with K_i values of 74.4 nM and 269.4 nM for ENO2 and ENO1, respectively. Hex is a NfENO and TbENO inhibitor with IC₅₀s value of 0.14 μM and 2.1 μM, respectively. Hex has antimalarial activity against Plasmodium falciparum 3D7, Naegleria fowleri trophozoites and Plasmodium berghei ANKA strain. Hex has anti-tumor effects against intracranial tumors.

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.

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.

Diclofenac (Standard) is the analytical standard of Diclofenac. This product is intended for research and analytical applications. Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

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.

Nizatidine is a potent and orally active histamine H₂ receptor antagonist, can be used for the research of stomach and intestines ulcers. Nizatidine works by decreasing the secretion of gastric acid the stomach makes and prevent ulcers from coming back after they have healed in animal models.

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.

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.

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.