Inflammation/Immunology

Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC₅₀s of 0.39 μM and 2.39 μM, respectively.

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.

Hydroxyfasudil is a ROCK inhibitor, with IC₅₀s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

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.

Simepdekinra (LY4100511; DC-853) is an IL-17A antagonist. Simepdekinra can be used in the research of moderate to severe plaque-type psoriasis.

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.

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

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

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.

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.

AZD1981 is the antagonist for GPR44 (also known also PTGDR2, DP2 or CRTh). AZD1981 blocks the binding of PGD2 to CRTH2. AZD1981 exhibits immunomodulatory effects and can be used in research of chronic spontaneous urticaria.

FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC₅₀ of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC₅₀s of 7.7 and 6.5 µM, respectively.

LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a K_d of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells.

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.

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.

Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC₅₀s of 77 nM and 6.49 μM, respectively.

Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate 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.

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.