Tibulizumab (LY 3090106) is a tetravalent bispecific monoclonal antibody targeting B-cell activating factor (BAFF) and IL-17A with Kd values of 60 pM and 14 pM, respectively. Tibulizumab can be used for autoimmune disease research[1].
Neocryptotanshinone, a fatty diterpenoids from Salvia Miltiorrhiza, inhibits lipopolysaccharide-induced inflammation by suppression of NF-κB and iNOS signaling pathways[1][2].
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95[1][2].
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.IC50 Value: 0.7 nM [1]Target: HPGDSHPGDS inhibitor 1 was elected for further profiling based on its enzyme and cell potency. The compound illustrated equal potency against purified HPGDS from human , rat, dog, and sheep (IC50, 0.5-2.3 nM). HPGDS inhibitor 1 was profiled in a panel of cellular assays to screen for activity against several relevant human enzyme targets. Those assay indicated that HPGDS inhibitor 1 does not inhibit human L- PGDS, m-PGDS, COX-1, COX-2 or 5 LOX (IC50 values > 10000 nM).HPGDS inhibitor 1 had a solubility of 1.5 ug/ml (3.9 uM) at pH 6.5. The compound had excellent PK characteristics when dosed in rats at 1 mpk with 76% bioavailavility. Rats dosed orally with 1 and 10 mpk HPGDS inhibitor 1 were sacrificed at various times, and plasma concentrations of HPGDS inhibitor 1 and spleen PGD2 concentrations were measured. Oral administration of HPGDS inhibitor 1 blocked PGD2 production in the rat spleen; inhibition of PGD2 was inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time and dose-dependent manner. Spleen PGD2 levels fall as HPGDS inhibitor 1 plasma levels increase over time; PGD2 levels return to baseline levels as HPGDS inhibitor 1 plasma levels decline.
E7766 disodium is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 disodium shows potent pan-genotypic and antitumor activities[1].
L-NABE is a nitric oxide (NO) synthase inhibitor. L-NABE is also a potent endothelium dependent vasoconstrictor and inhibitor of relaxation[1][2].
ABH (hydrochloride) is a potent arginase inhibitor. ABH (hydrochloride) can be used for researching anti-inflammation[1].
Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately[1].
PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC50 of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Mepolizumab (SB 240563) is a humanized monoclonal antibody that binds to and neutralizes interleukin-5 (IL-5), the major cytokine involved in eosinophil proliferation, activation, and survival. Mepolizumab can be used for the research of eosinophilic granulomatosis with polyangiitis (EGPA) and severe eosinophilic asthma[1][2].
IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity[1][2].
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2].
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis)[1].
H4R antagonist 3 (Example 18) is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. H4R antagonist 3 can be used for the research of prevention of inflammatory, autoimmune, allergic, and ocular diseases[1].
IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).IC50 value:Target: IFN alpha-IFNAR interaction inhibitorIFN alpha-IFNAR-IN-1 specifically inhibits MVA-induced IFN-α responses by BM-pDCs. IFN alpha-IFNAR-IN-1 inhibited the IFN-α responses that were elicited after treatment with CpG2216, stimulation with poly(I:C), and infection with VSV-M2, whereas the total IL-12 production was notably less affected under those conditions. IFN alpha-IFNAR-IN-1 exerts immunosuppressive activity by the direct interaction with IFN-α [1].
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity[1]. Metyrosine is a very effective agent for blood pressure control[2].
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function[1].
Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS)[1][2].
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research[1].
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.
Brompheniramine maleate is a histamine H1 receptors antagonist.Target: Histamine H1 ReceptorBrompheniramine maleate, is an antihistamine drug of the propylamine (alkylamine) class. It is readily available over the counter and is indicated for the treatment of the symptoms of the common cold and allergic rhinitis. It is a first-generation antihistamine. Brompheniramine has antidepressant properties, inhibiting reuptake of the neurotransmitter serotonin. Based on this knowledge, Arvid Carlsson and his colleagues, working at the Swedish company Astra AB, were able to derive the first marketed selective serotonin reuptake inhibitor, zimelidine, from brompheniramine. Brompheniramine had a long half-life and large volume of distribution in normal adults. It also had a prolonged antihistaminic effect in the skin as evidenced by suppression of the wheal and flare response to histamine and by suppression of pruritus [1, 2].
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively[1].
Juncutol is a potent inducible nitric oxide synthase (iNOS) inhibitor. Juncutol decreases the LPS (HY-D1056)-stimulated iNOS protein expression[1].
CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research[1].
L-Arginine-13C ((S)-(+)-Arginine-13C) hydrochloride is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
SLM6031434 hydrochloride is a highly selective sphingosine kinase 2 (SphK2) inhibitor with Kis of 0.4 μM, 0.5 μM, >20 μM, 22 μM for mSphK2, rSphK2, mSphK1 and rSphK1, respectively. SLM6031434 hydrochloride decrease Sphingosine 1-phosphate (S1P) levels in U937 monocytic leukemia cells. SLM6031434 hydrochloride has the potential for renal fibrosis research[1][2].
Dapansutrile (OLT1177) is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity[1].