immunotherapy

Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5).

SM-324405 is an agonist of TLR7.

EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

GW280264X (Carbamic acid) is an inhibitor of ADAM17 .

CH-223191 is a specific and effective aromatic hydrocarbon receptor (AhR) antagonist, and its IC50 value for inhibiting luciferase activity induced by TCDD is 0.03 μM. CH-223191 can be used in tumor immunotherapy, cytotoxicity research, stem cell research, inflammation research and neuroprotection.

Benzofuran-2-carboxylic acid, also known as LYxylic blue, is an inhibitor of multiple oxidase systems that can be used as a lymphotyrosine phosphatase (LYP) inhibitor for cancer immunotherapy.

BMS-986449 is an IKZF2 (Helios)/IKZF4 (Eos) degrader and CELMoD molecular glue. It redirects the interaction between the E3 ubiquitin ligase Cereblon and Helios/Eos in primary Treg cells, inducing their degradation, and may be utilised for anti-tumour immunotherapy.

BAY 2416964 is a small molecule inhibitor that selectively targets aromatic receptor (AhR) with an IC50 of 341 nM and is commonly used in cancer immunotherapy research.

Compound 3 (diABZI-V/C-DBCO) functions as an efficient STING agonist. This compound acts by releasing diABZI-amine under the action of cathepsin B to activate STING, thereby inducing the production of interferon and other immune-activating molecules, which enhances the immune system's response to tumors. In THP1-Dual cells, the EC50 values for STING activation by diABZI-V/C-DBCO and diABZI-amine are 1.47 nM and 0.144 nM, respectively, and in primary mouse splenic cells, the EC50 values are 7.7 µM and 0.17 µM, respectively. diABZI-V/C-DBCO is useful for research in the field of cancer immunotherapy.

XYL-1 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. It has the capability to enhance type I interferon signaling in vitro, positioning it as a potential candidate for the development of cancer immunotherapy drugs.

Lon-TK is a glycolysis inhibitor of LTB, linked with a linker conjugate. LTB is an intelligent responsive prodrug, comprised of Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1), which are connected through a thioketal linkage. It effectively inhibits glycolytic metabolism in tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK holds potential for use in photodynamic-enhanced immunotherapy research.

ERAP1-IN-3 (compound 13) is a potent inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1), with a pIC50 value of 8.6. ERAP1-IN-3 shows potential for research in cancer immunotherapy and autoimmune disease studies.

TLR7 agonist28 (compound 3) is a potent TLR7 agonist. This compound can be combined with anti-tumor monoclonal antibodies (mAb) for use in cancer immunotherapy.

Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and exhibits low oral bioavailability. By inhibiting cGAMP degradation, it effectively activates the intracellular STING pathway. Enpp-1-IN-25 can enhance immune cell infiltration and type I interferon response in the tumor microenvironment, thereby increasing the antitumor efficacy of anti-PD-L1 antibodies. It is applicable for research in cancer immunotherapy.

BTN3A1 ligand-1 (Compound 26b) is an aryl/acylalkyl phosphonate prodrug containing a triazole group. It is capable of stimulating T cell proliferation (EC50: 0.49 nM) and promoting interferon γ secretion. Additionally, this compound exhibits a degree of plasma stability, making it relevant for research in immunotherapy.

UNC8212 is a potent TAM kinase inhibitor. It exhibits strong inhibitory activity against MERTK and AXL, with IC50 values of 1.5 nM and 1.3 nM, respectively, and also inhibits TYRO3 with an IC50 of 6.7 nM. By targeting the structurally diverse "back-pocket" region within the TAM kinase family, UNC8212 modulates polypharmacology characteristics. It binds tightly to TAM kinases and effectively inhibits MERTK and AXL phosphorylation. UNC8212 possesses antitumor properties and is applicable in cancer immunotherapy and target studies for tumor cells.

HPK1-IN-57 (Compound 10c) is an inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of 0.09 nM. It suppresses the activity of HPK1 kinase, inhibits the phosphorylation of downstream adaptor protein SLP76 (IC50 of 33.74 nM), and effectively induces the secretion of the T cell activation marker IL-2 (EC50 of 84.24 nM). HPK1-IN-57 holds promise for research in tumor immunotherapy.

FGT-4 is a chimeric molecule targeting folate receptor β (FR-β) and functions as a TLR7 agonist. It enhances the secretion of iNOS and the pro-inflammatory cytokine IL-6 associated with M1 macrophages and promotes the proliferation of cytotoxic CD8+ T cells. FGT-4 demonstrates antitumor activity in the 4T1 breast cancer mouse model and is applicable for cancer immunotherapy research.

TBK1-IN-2 (Compound A1) is a potent inhibitor of TBK1 with an IC50 of 775 pM. It binds to TBK1 through stable hydrogen bonding and π-π stacking interactions, thereby inhibiting the phosphorylation of IRF3. TBK1-IN-2 works in synergy with TNF/IFNγ to enhance immune-mediated tumor cell death and is applicable in cancer immunotherapy research.

TP1L is a selective TC-PTP PROTAC degrader used in cancer immunotherapy, with a DC50 value of 35.8 nM.

endo-S-cGAFMP (Compound 3) is a STING agonist that enhances both innate and adaptive immune responses by activating the cGAS-STING pathway, leading to the production of interferon regulatory factors and pro-inflammatory cytokines. It exhibits strong immunostimulatory activity in THP1 monocytes and RAW macrophages, with EC50 values of 2.45 μM and 5.54 μM, respectively. endo-S-cGAFMP also demonstrates significant antitumor activity and holds potential as an immunotherapy agent for cancer, particularly in studies involving systemic administration.

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. It binds effectively to human and mouse PD-L1 proteins, exhibiting KD values of 171 nM and 290 nM, respectively. In a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells, GJ19 promotes HepG2 cell death in a concentration-dependent manner. In the B16-F10 melanoma mouse model, GJ19 demonstrates significant tumor growth inhibition. GJ19 is applicable in tumor immunotherapy research.

DF-006 is an innovative orally active agonist of ALPK1 (α-kinase 1). It stimulates the innate immune response in the liver by activating the NF-κB pathway. DF-006 effectively reduces serum levels of hepatitis B virus (HBV) DNA (EC50 = 2.7 pM), HBsAg, and HBeAg, demonstrating potent antiviral activity, making it suitable for immunotherapy research in chronic hepatitis B (CHB).