Inflammation/Immunology

Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with high affinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis.

Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia.

AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.

SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .

Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease.

Racotumomab (Anti-Human NGcGM3 Recombinant Antibody) is an anti-idiotype monoclonal antibody (MAb). Racotumomab reacts to Neu-glycolyl (NeuGc)-containing gangliosides, sulfatides, and other antigens expressed in tumors. Racotumomab is an active anticancer agent for lung cancer.

Flobufen (VUFB 16066) is a non-steroidal anti-inflammatory agent and cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor agent. Flobufen inhibits alloantigen-driven cellular immune responses and stimulates phagocytosis of peritoneal cells. Flobufen can improve immunopathological disorders and has an inhibitory effect on rheumatoid arthritis.

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC₅₀=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC₅₀ of 0.04 μM.

HY-P990926 is an SIRPA-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC₅₀ of 163 nM.

Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC₅₀=1.3 μM in human liver microsomes) and CYP2D6 (K_i=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.

HY-P990910 is an IL4R-targeting IgG4κ type humanized antibody, the recommed isotype control is Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Anti-Mouse CD117/c-Kit Antibody (2B8) is an IgG2b antibody, targeting to mouse CD117/c-Kit. Anti-Mouse CD117/c-Kit Antibody (2B8) reacts with mouse c-Kit (also known as CD117), which is expressed on hematopoietic progenitor cells, mast cells, and acute myeloid leukemia (AML) cells. Anti-Mouse CD117/c-Kit Antibody (2B8) can be used for the detection of flow cytometry, immunofluorescence and immunohistochemistry in cancer and inflammation.

GPR4 antagonist 1 is a GPR4 antagonist, with an IC₅₀ of 189 nM.

9-cis-Retinoic acid-d₅ is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

SGK1-IN-2 (Compound 14h) is a selective, ATP-competitive SGK1 inhibitor, with an IC₅₀ of 0.005 μM at 10 μM ATP and an IC₅₀ of 0.025 μM at 500 μM ATP. SGK1-IN-2 can be used in studies of cancer, hypertension and diabetes.

PSB 0777 ammonium hydrate is a potent and selective adenosine A_2A receptor full agonist with K_i values of 44.4 nM, 360 nM for rat and human A_2A receptors, respectively. PSB 0777 ammonium hydrate has K_i values of ≥10000 nM, 541 nM for rat and human A₁ receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research.

Ufenamate (Flufenamic acid butyl ester) is an anthranilic acid-based anti-inflammatory drug that can be used in the study of skin diseases such as acute and chronic eczema, contact dermatitis, diaper dermatitis, miliary rashes and atopic dermatitis. Ufenamate has a certain photoprotective effect, reduces the degree of skin erythema and swelling in the photoaging model, downregulates the expression level of COX-2 and can promote the healing of mouse skull defects by secreting BMP2.

FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC₅₀ = 3.2 nM; THP-1 cells: DC₅₀ = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC₅₀ = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis.

THR-123 TFA is an orally active ALK3 peptide agonist. THR-123 TFA has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 TFA suppresses inflammation, Apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 TFA can be used for the study of kidney fibrosis.