Robotnikinin is a small molecule capable of binding to and inhibiting the activity of Sonic Hedgehog (Shh) signaling up stream of Smo[1][2].
Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma[1][2][3].
LY 3000328 is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.
LS-102 is a selective synoviolin inhibitor (Syvn1). LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of ~15 μM. LS-102 has the potential for rheumatoid arthritis treatment[1][2].
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and drug-sensitive (DS) M. tuberculosis[1].
DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role[1].
Aurantimycin A (Adipogen), a depsipeptide antibiotic, displays strong activity against Gram-positive bacteria. Aurantimycin A is a substrate of the LieAB transporter[1][2].
K-80001 is an RXRα-binder and COX-1/2 inhibitor, with IC50s of with an IC50 of 82.9μM, 3.4μM, 1.2μM for RXRα, COX-1 and COX-2, respectively[1].
4-Hydroxyoxyphenbutazone kills both replicating and nonreplicating (NR) Mycobacterium tuberculosis (Mtb), including Mtb resistant to standard drugs. 4-Hydroxyoxyphenbutazone is a potent inhibitor of cytokine production. 4-Hydroxyoxyphenbutazone is an immunosuppressive drug and has the potential for rheumatoid arthritis research[1][2].
Cilomilast-d9 (SB-207499-d9) is the deuterium labeled Cilomilast. Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD)[1][2][3][4].
NLRP3 / aim2-in-2 is a new potent inhibitor with different species-specific effects on NLRP3 and aim2 inflammasome dependent cell death. Its < b > IC < sub > 50 < / sub > < / b > value is 0.2392 ± 0.0233 μ M。
CCR3 antagonist 1 is a potent antagonist of CCR3, used for the research of immunologic and inflammatory diseases.
6-keto Prostaglandin F1α is an endogenous metabolite present in Cerebrospinal_Fluid, Urine and Blood that can be used for the research of Meningitis, Rheumatoid Arthritis and Cardiopulmonary Resuscitation[1][2][3][4].
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM[1][2].
Eflapegrastim is a humanized IgG4 monoclonal antibody, is also a granulocyte colony-stimulating factor (G-CSF). Eflapegrastim targets to G-CSF receptor (c-Fms). Eflapegrastim stimulates proliferation and differentiation of neutrophil progenitor cells and maintains stable numbers of mature and functional neutrophils. Eflapegrastim also shortens the duration of neutropenia[1].
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1].
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola[1][2].
NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).IC50 value: 16/11 nM(Binding/Functional IC50) [1]Target: EBI2/GPR183 antagonistNIBR189 is a potent and selective EBI2 antagonist with improved pharmacokinetic properties which will help to probe the physiological function of EBI2 in health and disease.
JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
Antimalarial agent 16 (Compound 4h) is a parasite inhibitor. Antimalarial agent 16 shows antimalarial activity, and can inhibit P. falciparum parasite growth (IC50=2.0 nM)[1].
2'-C-Methyladenosine is an inhibitor of hepatitis C virus (HCV) replication. 2'-C-Methyladenosine inhibits HCV replicon and NS5B-catalyzed RNA synthesis with IC50 values of 0.3μM and 1.9 μM, respectively. 2'-C-Methyladenosine also potently inhibits LRV1 in Leishmania guyanensis (Lgy) and Leishmania braziliensis[1][2].
MCC950 sodium is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
C5 Lenalidomide (Lenalidomide 5'-amine) is a thalidomide analog and is a potent inhibitor of TNF-alpha production (IC50=100 μM in LPS stimulated human PBMC)[1].
Cromolyn sodium is an antiallergic drug.Target: Calcium ChannelCromolyn sodium is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.Pretreatment of IIR mice with Cromolyn sodium prior to ischemia exhibited no changes of ET-1 levels, injury score and inflammation (P>0.05, PreCr vs. M groups). In conclusion, administration of Cromolyn sodium after reperfusion, but not prior to ischemia, attenuates IIRI by downregulating ET-1 and suppressing sustained MC activation [1]. cromolyn sodium has a role in the prevention of Chronic lung disease(CLD). Cromolyn sodium cannot be recommended for the prevention of CLD in preterm infants [2].
Iso-PPADS tetrasodium is a P2X-purinoceptor antagonist. Iso-PPADS tetrasodium inhibits P2X1 and P2X3 receptor with IC50s of 43 nM and 84 nM. Iso-PPADS tetrasodium is protective against ventilator-induced brain injury (VIBI)[1][2].
ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities[1].
α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.
Placulumab (ART621) is an anti-TNF α monoclonal antibody. Placulumab has anti-inflammatory activity and has potential applications in inflammatory diseases such as arthritis[1].
AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2[1].