nod in 1

NOD-IN-1 (Compound 4) is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors.

NOD1/2 antagonist-1 is a dual inhibitor of nucleotide-binding oligomerization domain-like receptors NOD1 and NOD2, exhibiting IC50 values of 1.13 uM for NOD1 and 0.77 uM for NOD2, with an acceptable half-life of 67.6 minutes. NOD1/2 antagonist-1 enhances the antitumor efficacy of paclitaxel and serves as a potent experimental tool for investigating innate immune receptor-mediated signaling and cancer therapy modulation.

NOD1/2-IN-1 (Compound 18) is a potent RIPK2 inhibitor, demonstrating an IC50 value of 1.4 nM in the ADP-Glo assay. It blocks the production of pro-inflammatory cytokines by inhibiting the NOD1/NOD2 pathway (IC50 values are 18 nM and 170 nM for NOD1 and NOD2, respectively), thereby reducing inflammatory responses. This compound is utilized in research related to colitis.

NOD1/2-IN-1 (Compound 2) is a potent inhibitor of RIPK2 with an IC50 value of 0.65 nM as determined by the ADP-Glo assay. It selectively inhibits the NOD1 pathway, with an IC50 of 33 nM, effectively blocking the production of pro-inflammatory cytokines and thereby reducing inflammatory responses. This compound has potential applications in the research of colitis.

NOD2 agonist 1 (compound 3) is a potent NOD2 activator with an EC50 of 4.6 nM.

NOD1-RIPK2-IN-1 (Compound 37) is an inhibitor of the NOD1-RIPK2 signaling pathway, displaying potent IC50 values of 42 nM and 1.52 nM against NOD1 and RIPK2, respectively. This compound effectively reduces the secretion of the pro-inflammatory cytokine IL-8, making it valuable for research in inflammation and immune disorders.

NOD1antagonist-2 (compound 66) is an orally active and selective inhibitor that can suppress NOD1 in both humans and mice. It effectively blocks the NOD1-induced NF-κB and MAPK pathways.

NOD1antagonist-1 (compound 37) acts as an antagonist to NOD1 and exhibits a slight selectivity between NOD1 and NOD2, with IC50 values of 9.18 μM and 20.8 μM, respectively.

NOD2/TLR4 agonist-1 (Compound 2) is a dual agonist for NOD2 and TLR4. It does not possess immunostimulatory activity, making it a significant negative control in research studies.

NOD2 antagonist 1 (compound 32) is an effective and selective NOD2 antagonist (IC50: 5.23 μM). In THP-1 cells, it represses Muramyl DiDP (MDP)-induced IL-8 secretion and, in PBMCs cells, inhibits MDP-induced elevation of IL-6, IL-10, and TNF-α.

AC1NOD4Q is a novel blocker of hox antisense intergenic rna (hotair) by abrogating the scaffold interaction with ezh2

APD-94 is a dual inhibitor targeting tubulin and Bmi-1. It disrupts the normal polymerization of tubulin and suppresses the expression of Bmi-1. This compound induces cell cycle arrest at the G2/M phase and triggers apoptosis, thereby inhibiting cancer cell proliferation. Additionally, APD-94 inhibits the growth of HT29 cell xenograft tumors in NOD/SCID mice and is applicable to colorectal cancer research.

PROTACFLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader targeting FLT3, JAK2, and BRD4, with DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It exhibits potent antiproliferative activity against MV4;11 cells (IC50= 0.79 nM) and FLT3-mutated Ba/F3 cells. Additionally, PROTACFLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells and demonstrates significant antitumor efficacy in an MV4;11 xenograft model established in NOD SCID mice. This compound is applicable for research in acute myeloid leukemia (AML).

NLRP3-IN-9 (INF-4E) is an inhibitor of NLRP3 ATPase and caspase-1. NLRP3-IN-9 acts by irreversibly trapping thiol nucleophiles, which prevents both ATP- and nigericin-triggered pyroptosis of human THP-1 cells in a time- and concentration-dependent manner.

FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits glucose-induced increases in prostaglandin E2 production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.

AD4 is an artemisinin-derived proteolysis targeting chimera that selectively degrades PCLAF protein with subnanomolar potency in RS4;11 leukemia cells,AD4 leads to activation of the p21/Rb signaling axis, robust anti-tumor activity, and significantly prolonged survival in RS4;11 xenograft NOD/SCID mouse models, demonstrating both in vitro and in vivo therapeutic efficacy.

GAD65 (524-543) is a biologically active peptide comprising amino acids 524 to 543 of glutamic acid decarboxylase 65 (GAD65). It represents an early islet antigen fragment that elicits proliferative T cell responses in the non-obese diabetic (NOD) mouse model, instrumental in spontaneous autoimmune diabetes research. The peptide serves as a specific, possibly low-affinity stimulant for the diabetogenic T cell clone BDC2.5. Notably, immunization with GAD65 (524-543) heightens NOD mice's vulnerability to type 1 diabetes when subjected to the adoptive transfer of BDC2.5 T cells.

DiaPep277, a 24 amino acid peptide sourced from HSP60 positions 437-460, impedes β-cell destruction in NOD mice and modulates diabetogenic T-cell activity in animal diabetes models [1] [2].

NLRP3-IN-38 (Compound 18) serves as an inhibitor of the NOD-like receptor protein 3 (NLRP3), effectively blocking the activation of the NLRP3 inflammasome with an EC50 value of 23 nM [1].

Tregitope 289 is a peptide derived from the Fc region of immunoglobulin G (IgG) and serves as a highly conserved T cell epitope that promotes the expansion of natural regulatory T cells. When co-delivered with type 1 diabetes (T1D) antigens, it can delay the onset of hyperglycemia and reduce the incidence of diabetes in NOD mouse models. Tregitope 289 is applicable for research in T1D and other autoimmune diseases.