Cancer Immunotherapy

Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC₅₀s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC₅₀ of 3 μM. Staurosporine is an apoptosis inducer.

5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.

Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).

Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.

Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A inhibits HSV-1 and has anti-cancer activity.

Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.

Streptozotocin (Streptozocin; STZ) is an antibiotic widely used in experimental animal models of induced diabetes. Streptozotocin enters B cells via the glucose transporter (GLUT2) and causes the alkylation of DNA ( DNA-methylating ). Streptozotocin can induce the apoptosis of β cells.

Bleomycin sulfate is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin sulfate is an antitumor antibiotic.

BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC₅₀=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC₅₀s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.

Lactic acid (DL-Lactic acid) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid is an oncometabolite and has immune protective role of lactate in anti-tumor immunity. Lactic acid also has antimicrobial activity, which can be used as a food preservative.

Lactic acid (DL-Lactic acid) sodium (60% w/w in water) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium (60% w/w in water) is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium (60% w/w in water) is an oncometabolite and has immune protective role of lactate in anti-tumor immunity. Lactic acid sodium (60% w/w in water) also has antimicrobial activity, which can be used as a food preservative.
This product has a content (w/w) of 60%, and 1 mL of the system contains 798 mg of Lactic acid sodium, i.e., a concentration of 798 mg/mL (i.e., 7.12 M).

DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC₅₀s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ₄₂, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.

CCCP is an oxidative phosphorylation (OXPHOS) uncoupler. CCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation.

Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Puromycin dihydrochloride (CL13900 dihydrochloride), an aminonucleoside antibiotic, inhibits protein synthesis.

Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC₅₀ of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC₅₀=182 nM). Necrostatin-1 is also an IDO inhibitor.

Human IgG1 kappa, Isotype Control is a human monoclonal antibody that is the isotype control of human IgG1 kappa antibody.