Inflammation/Immunology

nor-NOHA acetate is a selective and reversible Arginase inhibitor. nor-NOHA acetate induces Apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA acetate has anti-leukemic activity. nor-NOHA acetate improves liver ischemia-reperfusion injury. nor-NOHA acetate can used in study of tuberculosis, endothelial dysfunction, immunosuppression and metabolism.

BMS-986408 is an orally active inhibitor of DGKα and DGKζ, with IC₅₀ values of 0.0003 μM and 0.002 μM, respectively. BMS-986408 activates intratumoral T cell responses, enhances the priming and expansion of tumor-reactive T cells in tumor-draining lymph nodes, and functions as an immunostimulant. BMS-986408 can be used in the research of tumors.

Cadefrecitinib (GLPG3667) is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC₅₀ of 2.3 nM. Cadefrecitinib inhibits IFNα/pSTAT1, and the IC₅₀ values ​​in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. Cadefrecitinib has the potential for the study of inflammatory and autoimmune diseases.

IL-15-IN-1 (compound 76) is a potent and selective Interleukin 15 (IL-15) inhibitor, inhibiting the proliferation of IL-15-dependent cells with an IC₅₀ of 0.8 μM.

PKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase Cθ (PKCθ), with a K_i value of 6 nM. PKC-theta inhibitor 1 inhibits T-cell-mediated inflammatory responses by suppressing the release of proinflammatory cytokines (IL-2 IC₅₀ = 0.21 μM in anti-CD3/CD28-stimulated PBMCs; IL-17 IC₅₀ = 1 μM in CD3/CD28-stimulated Th17 cells) PKC-theta inhibitor 1 significantly reduces symptoms in mice with ongoing experimental autoimmune encephalomyelitis (EAE). PKC-theta inhibitor 1 can be used for the study of T-cell-mediated inflammatory diseases such as multiple sclerosis.

MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.

Vapendavir diphosphate (BTA798 diphosphate) is a potent enteroviral capsid binder (CB). Vapendavir diphosphate (BTA798 diphosphate) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC₅₀ values of 0.5-1.4 μM in different EV71 strains.

Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC₅₀: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .

Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM.

WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC₅₀ of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.

Charybdotoxin TFA, a 37-amino acid peptide, is a K⁺ channel blocker.

Anti-Mouse TNFR2 Antibody (TR75-54.7) is an anti-mouse TNFR2 IgG monoclonal antibody. Anti-Mouse TNFR2 Antibody (TR75-54.7) can reduce white blood cell count (WBC) and decrease the expression of some pro-inflammatory cytokines such as CCL2 and CXCL5. Anti-Mouse TNFR2 Antibody (TR75-54.7) can be used for researches on inflammation conditions and cancer such as breast cancer.

SR12418 is a REV-ERB-specific synthetic ligand with IC₅₀s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.

Eliapixant (BAY 1817080) is a potent and selective antagonist of P2X3 receptor, with an IC₅₀ of 8 nM. Eliapixant can be used for the research of refractory chronic cough.

Bexmarilimab (FP-1305) is a potent humanized anti-CLEVER-1 IgG4 antibody with an IC₅₀ value of 4.51 nM. Bexmarilimab is capable of inducing a phenotypic M2 to M1 immune switch of tumor-associated macrophages. Bexmarilimab can promote antigen presentation and pro-inflammatory cytokine secretion. Bexmarilimab can induce B-cell and T-cell activation. Bexmarilimab can be used in researches of immunology and cancer, such as colorectal carcinoma.

Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation.

Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC₅₀s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.

Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs).

Thromboxane B2 is a prostaglandin derivative that is released during anaphylaxis. Thromboxane B2 induces arterial contraction and platelet aggregation. Thromboxane B2 is a biological inactive product and circulating catabolite of thromboxane A2. Thromboxane B2 levels in peripheral venous blood and coronary sinus blood can be used as a diagnostic marker for angina. Thromboxane B2 level in serum is also associated with inhibition of COX-1 activity inhibition in platelets. Thromboxane B2 is a major product of prostaglandin endoperoxide metabolism. Thromboxane B2 produces dose-related decreases in airflow rate, tidal volume and dynamic lung compliance, whilst simultaneously increasing pulmonary airway resistance in dog model. Thromboxane B2 appears to be a naturally occurring bronchoactive metabolite in the bioconversion of arachidonic acid.

LT052 is a highly selective BET BD1 inhibitor with an IC₅₀ of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC₅₀=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research.