Inflammation/Immunology

Venanprubart is an anti-BTLA human IgG4 κ monoclonal antibody. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Rapamycin (Sirolimus) GMP Like is Rapamycin (HY-10219) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.

ZN-A-1041 inhibits HER2 in BT474 cell and wt-EGFR in H838 cells, with IC₅₀s of 9.5 nM and 12 μM respectively. ZN-A-1041 can be used for research of cancer and inflammation.

GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC₅₀s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.

P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC₅₀s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.

Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC₅₀ of 222 μM.

Gersizangitide (AXT107) is an anti-angiogenic peptide consisting of 20 amino acids, derived from collagen IV. Gersizangitide is an inhibitor of VEGF-A and VEGF-C and an activator of Tie2. Gersizangitide can block VEGF receptor signaling, inhibit vascular leakage, neovascularization and inflammation. Gersizangitide can be used in the research of diseases related to ocular neovascularization and angiogenesis.

KPLH1130 is a pyruvate dehydrogenase kinase (PDK) inhibitor. KPLH1130 potently inhibits M1 macrophage polarization by reducing the expression of pro-inflammatory cytokines, decreasing the levels of M1 phenotype markers (HIF-1α, iNOS) and nitric oxide (NO) production. KPLH1130 prevents the reduction of mitochondrial oxygen consumption rate (OCR) induced by inflammatory stimuli (LPS ((HY-D1056) + IFN-γ) in various macrophage types. KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 can be used for the study of obesity-associated metabolic disorders and other inflammatory conditions.

Loxoprofen sodium is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC₅₀s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium can reduce atherosclerosis and shows antitumor activity.

ABBV-712 is a selective and orally active inhibitor of Tyrosine kinase 2 (TYK2). ABBV-712 has EC₅₀ values of 0.01, 0.19, and 0.17 μM for TYK2 JH2, TYK2 cells and human whole blood, respectively. ABBV-712 has anti-inflammatory activity and can be used in the research of autoimmune diseases.

Lixumistat (IM156 free base) is a potent and orally active AMPK activator and OXPHOS inhibitor. Lixumistat strongly activates AMPK, while it lacks the systemic metabolic regulatory effects of classic metformin, such as hypoglycemic and weight-lowering activities. Lixumistat exhibits significant therapeutic effects on cognitive decline associated with brain aging and pulmonary fibrosis.

L-Histidine-¹³C₆ (hydrochloride hydrate) is the ¹³C-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable.

GSK-5498A is a selective CARC channel inhibitor (IC₅₀: 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders.

Tilpisertib fosmecarbil TFA (GS 5290 TFA) is a potent serine/threonine kinase inhibitor. Tilpisertib fosmecarbil TFA has anti-inflammatory activity.

biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models.

Emapticap pegol (NOX-E36) is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide pegylated aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36). mNOX-E36 is a murine-specific analogue of NOX-E36, an anti-MCP-1 L-RNA aptamer that was previously shown to attenuate liver fibrosis in mice.

Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with an IC₅₀ of 2.4 nM, compound 33, sourced from patent WO2018212534A1.

Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC₅₀s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.

Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC₅₀=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

Linvencorvir (RG7907) is an orally active Hepatitis B virus core protein allosteric modulator. Linvencorvir induces Apoptosis. Linvencorvir has antiviral activity against HBV.