TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM[1].
Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity[1][2].
ALPK1-IN-2 (compound T001) is a potent ALPK1 (alpha-kinase 1) inhibitor, with an IC50 of 95 nM. ALPK1-IN-2 also inhibits NF-κB, with an IC50 of 1.31 μM[1].
QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18[1][2][3].
7-Acetyllycopsamine, a pyrrolizidine alkaloid, is a mild hepatotoxin. 7-Acetyllycopsamine can induce liver inflammation in mice[1].
cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration[1][2]. MDL-28170 also block γ-secretase[4].
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
1-Tetradecanol, isolated from Myristica fragrans, is a straight-chain saturated fatty alcohol. 1-Tetradecanol possesses antibacterial and anti-inflammatory (periodontitis) activity[1].
Zovostotug is a human CD163 (scavenger receptor cysteine-rich (SRCR) type 1 M130) mAb[1].
Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab can be used for the research of cancer and fibrotic diseases [1].
Genipin 1-β-D-gentiobioside (Genipin 1-gentiobioside) is one of the most abundant and bioactive iridoid glycosides in Gardenia jasminoides Ellis, which possesses hepatoprotective, anti-inflammatory, antioxidant, and antithrombotic activities.
Tofacitinib citrate is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
VHLTP is the N-terminal pentapeptide of human hemoglobin beta. VHLTP binds to cell membranes and serves as a ligand for anti-HbA1c antibodies[1].
IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
Lumbokinase capsules attenuates myocardial ischemia-reperfusion (I-R) injury through the activation of Sirt1 signaling, and thus enhances autophagic flux and reduces I-R-induced oxidative damage, inflammation and apoptosis[1].
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity[1].
Canophyllal is a triterpene that can be isolated from the leaves of Elsholtzia ciliata. Canophyllal weakly inhibits the production of NO[1].
Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin inhibits LT formation in human whole blood (IC50 = 10 µM) and reduces LTB4 levels in the rat pleurisy model[1].
(R,R)-Palonosetron Hydrochloride is the active enantiomer of Palonosetron.
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen[1].
Begelomab (SAND-26) is a murine IgG2b monoclonal antibody against DPP-4/CD26. Begelomab can be used for the research of severe refractory idiopathic inflammatory myopathy[1][2].
(+)-Thienamycin is a potent broad-spectrum antibacterial and β-lactamase inhibitor that can be from Streptomyces cattleya[1].
IL-17 modulator 3 is an IL-17 modulator (US20200247785A1). IL-17 modulator 3 can be used for the research of inflammation, cancer and autoimmune diseases[1].
Zuvotolimod is a myeloid cell agonist compound-linker for antibody conjugate. Zuvotolimod can be used in the research of cancer and hepatitis[1][2].
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist[1].
Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar[1].
JNJ-17156516 is a你orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist[1].
AN-12-H5 is a bifunctional, enviroxime-like anti-Enterovirus compound that inhibits replication and the early stage of enterovirus 71 infection with EC50 of 0.55 uM; mutations in capsid proteins (G3112A, VP1-Ala224Thr, and G2396A, VP3-Arg227Lys mutations) are resistant to AN-12-H5.
HS220 (HS-220) is a Plasmodium-selective takinib analog that targets atypical P. falciparum protein kinase 9 (PfPK9, Kd=4.1 uM) but does not inhibit HsTAK1, decreases K63-linked ubiquitination in P. falciparum; inhibits P. berghei parasite load in HuH7 cells with EC50 of 43 uM, with no significant change on HuH7 viability; induce a unique phenotype where parasite size in hepatocytes increases.
Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent[1].