Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis[1].
Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect[1][2].
Terfenadine is a potent open-channel blocker of hERG with a mean IC50 of 204 nM.IC50 value: 204 nMTarget: HERGTerfenadine normally undergoes extensive first-pass metabolism in the liver to produce an active acidic metabolite. Terfenadine is a widely used, over-the-counter drug to treat allergies.
TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays.
DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF)[1].
HG-12-6 is a small-molecule inhibitor that bind preferentially to unphosphorylated IRAK4 with IC50 of 165.1 nM, displays 15-fold selectivity over phosphorylated IRAK4 (IC50=2876 nM); binds as type II inhibitor with IRAK4 in a “DFG-out” conformation.
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs)[1].Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy[2].
NOX2-IN-1 (compound 10) is an inhibitor of nicotinamide adenine dinucleotide phosphate oxidase isoform 2 (NOX2). NOX2-IN-1 targets the p47phox−p22phox protein−protein interaction with favorable binding affinities and cellular activities[1].
Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
Ginsenoside Rh8 is a saponin composition of roots of Panax ginseng. Ginsenosides are the major active pharmacological components of ginseng[1][2].
Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect[1][2][3][4][5][6][7].
Pedunculagin is a potent 5α-reductase type 1 inhibitor. Pedunculagin inhibits nitric oxide (NO), IL-6, IL-8 production. Pedunculagin decreases the protein expression of 5α-reductase. Pedunculagin shows anti-inflammatory activity[1].
sRANKL-IN-2 (Compound S3-05) is a selective and orally active soluble RANKL (sRANKL) inhibitor with an IC50 of 0.41 μM. sRANKL-IN-2 can be used for the research of osteoporosis[1].
BTK-IN-20 (compound 283) is a BTK tyrosine kinase inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. BTK-IN-20 can be used for the research of cancer and inflammation[1].
(-)-Anomalin ((-)-Praeruptorin B) is a coumarin derivative isolated from the root of S. resinosum[1].
Licraside is isolated from Glycyrrhiza uralesis Fish.
AZD9056 is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca2+ influx and intracellular Ca2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice[1][2].
SB-273005 is a potent nonpeptide and orally active integrin antagonist with Kis of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively[1].
Deschloro Cetirizine Dihydrochloride is a Cetirizine impurity. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.
Clavulanic acid is a naturally occurring powerful bacterial β-lactamases inhibitor for research of infections caused by bacteria, including infections of the ears. Clavulanic acid is active against a wide spectrum of gram-positive and gram-negative bacterias[1].
Dimeric coniferyl acetate is a NO production inhibitor with an IC50 value 7.9 μM in BV-2 microglial cells[1].
18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
Thapsigargicin (Thapsigargicine) is a activator of mast cells and leukocytes. Thapsigargicin induces histamine release from rat peritoneal mast cells and human basophil leukocytes. Thapsigargicin increases the cytoplasmic free calcium level in intact human blood platelets[1].
(S,S)-TAPI-1 is an isomer of TAPI-1. TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor[1][2].
Bullatantriol ((+)?-?Bullatantriol) can be isolated from the roots of Homalomena aromatica. Bullatantriol can promote the proliferation and differentiation of osteoblasts. Bullatantriol also inhibits LPS-induced NO production in BV2 cells[1].
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively[1]. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA)[2].
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively[1].
SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM.