Inflammation/Immunology

LD03-DEX is a precursor compound of dexamethasone (HY-14648) with immunosuppressive activity.

Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31), is used as protein kinase C substrate peptide for testing the protein kinase C activity.

Landiolol-d₈ (ONO1101-d₈) is the deuterium labeled Landiolol (HY-100607). Landiolol (ONO1101) is a highly selective, ultra-short-acting competitive inhibitor of β₁ adrenergic receptors. Landiolol specifically blocks cardiac β₁ receptors, reducing heart rate and myocardial oxygen consumption. Landiolol inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol has little effect on cardiac ion channels (such as L-type calcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury.

MMT3-72 is a weak inhibitor of JAK1. MMT3-72 has superior efficacy and reduced p-STAT3 in DSS-induced colitis.

G9a ligand-1 is a target protein ligand that targets G9a, and it can be used in PROTAC-related research, such as serving as the PROTAC target protein ligand for PROTAC G9a degrader-1 (HY-187214).

CAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with K_i values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. CAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.

Idesin is a compound found in the fruits of Idesia polycarpa. Idesin inhibits LPS (HY-D1056)-induced nitric oxide production with mild cytotoxicity.

Quinotolast is an orally active antiallergic agent. Quinotolast inhibits histamine release from rat peritoneal cells. Quinotolast inhibits cutaneous cromoglycate in guinea pig model. Quinotolast has inhibitory effect on histamine and peptide leukotrienes release from guinea pig lung fragments and mouse cultured mast cells. Quinotolast can be studied in allergy-related research.

Etazolate (SQ 64442) is a α-secretase activator, selective PDE4 inhibitor, selective GABA_A receptor modulator. Etazolate reduces IL-1β levels Etazolate exerts a dose-dependent anti-inflammatory and anti-œdematous effect accompanied by lasting memory improvement. Etazolate produces an antidepressant-like effect.

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).

RXFP1 receptor agonist-5 (Example 98) is a RXFP1 receptor agonist. RXFP1 receptor agonist-5 stimulates cAMP production in HEK293 cells stably expressing human RXFP1, with an EC₅₀ value of 1.3 nM.

Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC₅₀s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis.

ATTO 488 streptavidin is a fluorescent reagent that specifically targets and binds to biotin (biotin), formed by the conjugation of ATTO 488 with streptavidin (HY-P3152). ATTO 488 streptavidin enables visualization of the activity of streptavidin immobilized on the surface of polymeric nanoparticles, or acts as a fluorescent probe to detect the selective binding and internalization process of anti-HB-EGF/NA with cells expressing HB-EGF (with no such effect on cells that do not express this receptor). ATTO 488 streptavidin effectively verifies the function of streptavidin conjugated to the surface of nanoparticles and is suitable for research related to atherosclerotic cardiovascular diseases.

sEH inhibitor-6 (Compound 3g) is a soluble epoxide hydrolase (sEH) inhibitor with an IC₅₀ of 0.5 nM.

Dimethyl diacetyl cystinate (DACDM) is a potent NF-κB inhibitor. Dimethyl diacetyl cystinate shifts the intracellular redox balance toward the oxidized state by increasing intracellular oxidized glutathione (GSSG) content, competitively blocking the binding of activated NF-κB to DNA, thereby inhibiting the production of inflammatory factors such as IL-1κ. Dimethyl diacetyl cystinate is promising for research of UVB-induced skin inflammation and related oxidative stress diseases.

PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC₅₀s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases.

BIO-11006 is a peptide that inhibits the function of the MARCKS protein. BIO-11006 attenuates LPS-induced neutrophil influx into the lungs, NF-κB activation, and expression of the proinflammatory cytokines KC and TNF-α. BIO-11006 also reverses disease progression in an LPS-induced mouse lung injury model. BIO-11006 is indicated for research on acute lung injury/acute respiratory distress syndrome (ALI/ARDS).

[Dehydro-Pro4] Substance P (4-11) is a peptide fragment of Substance P. Substance P is a peptide mainly secreted by neurons. Substance P takes part in many biological processes, including nociception, inflammation and immunity.

BMS-960 free base is a potent and selective S1P₁ receptor agonist containing isoxazole, which can be used in the research of immune diseases and vascular diseases.

Cortisone-¹³C₃ is the ¹³C-labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.