Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3[1].
Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8[1][2].
Myelin Oligodendrocyte Glycoprotein (40-54), Rat, Mouse (MOG (40-54)) is a CD8-related self-antigenic epitope of the myelin oligodendrocyte glycoprotein (MOG) protein and is presented in association with H-2Db[1].
Isoflupredone acetate is a corticosteroids with anti-inflammatory activity. Isoflupredone acetate can be used for research ketosis, musculoskeletal disorders, hypersensitivity, infections, inflammatory diseases in cows, horse, pigs, et al.[1][2].
Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.
AZD-8309 (AZD8309) is a potent and orally bioavailable CXCR2 antagonist that has been proposed to regulate the transmigration of neutrophils; significantly reduces MPO in the pancreas and lungs, and reduces intrapancreatic trypsin and elastase activity in caerulein-pancreatitis; also reduces cathepsin B activity and MPO in taurocholate-pancreatitis; also antagonises the CCR2b receptor but it is 10-fold less potent than at CXCR2. COPD Phase 1 Clinical
Tetrandrine is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca2+ current (ICa) and Ca2+-activated K+ current.
A potent PD-1/PD-L1 interaction inhibitor with IC50 of 80 nM in a homogenous time-resolved fluorescence binding assay.
3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) is a xanthone compound, with . 3-Hydroxyxanthone inhibits NADPH-catalysed lipid peroxidation in human umbilical vein endothelial cells (HUVECs). 3-Hydroxyxanthone also inhibits TNF-alpha induced ICAM-1 expression[1].
AM-8191, a bacterial topoisomerase inhibitors, has broad-spectrum antibacterial activity.
Furaltadone L-tartrate (Altafur L-tartrate), a nitrofuran drug, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci [1][2].
Angiotensin amide ((Asn1,Val5)-Angiotensin II) is a potent vasoconstrictor. Angiotensin amide is a derivative of angiotensin II. Angiotensin amide can be used as a cardiac stimulant[1].
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04)[1].
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research[1][2][3].
Amphotericin B trihydrate, a polyene antibiotic, is first isolated from fermenter cultures of Streptomyces nodosus. Amphotericin B trihydrate also possesses antileishmanial activity[1][2].
Bucillamine (SA96) is an orally active and potent sulfhydryl donor and antioxidant. Bucillamine is also an antirheumatic agent with antiangiogenic properties. Bucillamine can protect against Ischemia/reperfusion (I/R) injury in high-risk organ transplants. Bucillamine inhibits the production of VEGF. Bucillamine can be used for the research of choroidal neovascularization (CNV) and rheumatoid arthritis (RA)[1][2].
Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. IC50 value:Target: p38MAPKskepinone-L, the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chem. biol. research, and it may foster the development of a unique class of kinase inhibitors.
Ginsenoside Rg4 is a major protopanaxatriol type ginsenoside isolated from the leaves of Panax ginseng C. A. Meyer. The protopanaxatriol type ginsenosides (such as Ginsenoside Rg4) exhibits various biological activities including anti-septic, anti-diabetic, wound healing, immune-stimulatory, and anti-antioxidant activity[1][2].
CR4056 is a selective inhibitor of human recombinant MAO-A with an IC50 of 202.7 nM. CR4056 is also a ligand of imidazoline-2 receptor (I2R) with an IC50 of 596 nM.
Secoisolariciresinol diglucoside is a plant lignan isolated from flaxseed, an antagonist of platelet activating factor-receptor, and used as an antioxidant.
FPL59360 is a new Anti-asthmatic agent.
HPK1-IN-16 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-16 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019051199A1, compound 39)[1].
2,5-Di-tert-butylhydroquinone (DTBHQ), the indirect food additive, regulates the activity of 5-lipoxygenase as well as the activity of COX-2 (IC50=1.8 and 14.1 μM for 5-LO and COX-2, respectively) [1].
P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes[1].
cis-INCB3344 is the inactive isomer of INCB3344 (HY-50674), and can be used as an experimental control. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
(+)-Hannokinol can be isolated from AMOMUM TSAO-KO (ginger family) fruit. (+)-Hannokinol inhibits lipopolysaccharide-induced nitric oxide production in BV2 microglia[1].
Jh-X-119-01 is a novel potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 irreversibly labels IRAK1 at C302. This compound exhibited cytotoxic activity at single digit micromolar concentrations in a panel of WM, DLBCL, and lymphoma cell lines expressing MYD88. Cotreatment of JH-X-119-01 with the BTK inhibitor ibrutinib resulted in synergistic killing effects in these systems.
Tebotelimab (MGD-013) is a human IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity[1][2][3].
4,2'-Dihydroxy-4'-methoxychalcone, a chalcone, shows allergy-preventive effects[1].
Pateclizumab (MLTA3698A) is a humanized antibody against lymphotoxin α (LTα), a transiently expressed cytokine on activated B and T cells (Th1, Th17), which are implicated in rheumatoid arthritis (RA) pathogenesis[1].