Catalog No.
Product Name
Application
Product Information
Citations
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NOS cofactor
Biopterin is the oxidized form of tetrahydro-L-biopterin (BH4), a nitric oxide synthase (NOS) cofactor. L-Biopterin can be reduced to BH4 via thioredoxin reductase followed by dihydropteridine reductase or reduced glutathione. It is extremely toxic to human melanocytes in culture (IC50 = 0.2 uM after 48 hrs). -
Integrin agonist
Leukadherin 1 is an allosteric activator of CD11b/CD18. Increases CD11b/CD18-dependent cell adhesion to fibrinogen (EC50 = 4 μM). - Ecabet sodium is a widely employed mucoprotective agent for the treatment of gastric ulcers.
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DPP-IV inhibitor
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM). -
Thrombopoietin(TPO) receptor agonist
Avatrombopag is a novel orally-active thrombopoietin (TPO) receptor agonist. -
CXCR2 antagonist
SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury. - Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
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TLR7 agonist
Isatoribine is a novel guanosine analogue showing immunostimulatory activity both in vivo and in vitro. -
Nrf2 inhibitor
RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-kB. -
NOX1/4 inhibitor
GKT137831 is a first in class inhibitor targeting NOX1 and NOX4 enzymes.- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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hPGDS inhibitor
SAR191801 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay. - Benzydamine Hcl is a locally-acting nonsteroidal anti-inflammatory drug with local anaesthetic and analgesic properties; selectively binds to prostaglandin synthetase and has notable in vitro antibacterial activity.
- Anti-Inflammatory Peptide 1, belongs to the group of synthetic oligopeptides corresponding to a region of high amino-acid sequence similarity between uteroglobin and lipocortin I.
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CXCR4 antagonist
AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. -
c-mpl (TpoR) receptor agonist
Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis. -
CCR2 antagonist
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2. -
FLAP inhibitor
MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.- MA Sartim, .et al. , Biomolecules, 2020, May; 10(5): 794 PMID: 32443924
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COX-1 Inhibitor
Paradol is the active flavor constituent of the seeds of Guinea pepper (Aframomum melegueta); Paradol has been found to have antioxidative and antitumor promoting effects- Taurin Hughes, .et al. , Int J Biol Macromol, 2021, Jul 1;182:2130-2143 PMID: 34087308
- Lihan Zhao, .et al. , Sci Rep, 2020, Nov 5;10(1):19182 PMID: 33154433
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CXCL8 receptor inhibitor
Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models. -
CXCR2/CXCR1 antagonist
SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist. -
TLR4 Inhibitor
S enantiomer of TAK-242. TAK-242 (Resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling. TAK-242 is in treatment of sepsis and septic shock. - Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system.
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CCR5 antagonist
Vicriviroc maleate is a CCR5 antagonist with IC50 of 0.91 nM in clinical development for the treatment of HIV-1. -
NFAT inhibitor
NFAT Inhibitor, selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT).- Jingwen Liu, .et al. , Cell Mol Gastroenterol Hepatol, 2021, Jul 1;S2352-345X(21)00135-1 PMID: 34217895
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T cell activator
beta-Interleukin I (163-171), human, a peptide. Interleukins are a group of cytokines (secreted proteins/signaling molecules) that were first seen to be expressed by white blood cells (leukocytes). -
Immunomodulators
Cyclosporin B is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection. -
Calcineurin inhibitor
Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation. -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
anti-cancer agent
Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects. -
Immunomodulator
Aceneuramic acid is an immunomodulator potentially for treatment of hereditary inclusion body myopathy (HIBM). -
Calcineurin/PP2B inhibitor
Ascomycin is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It has been researched for the treatment of autoimmune diseases and skin diseases, and to prevent rejection after an organ transplant. -
TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.- Angelina T Regua, .et al. , Cancer Lett, 2024, Jun 7:597:217023 PMID: 38852701
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Analog of curcumin
Dimethoxycurcumin, a synthetic curcumin analogue with higher metabolic stability, inhibits NO production, inducible NO synthase expression and NF-kappaB activation in RAW264.7 macrophages activated with LPS. -
FLAP inhibitor
GSK2190915 is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.
