Tomaralimab (OPN-305) is a humanised anti-TLR2 IgG4 monoclonal antibody. Tomaralimab has the potential for the research of Myelodysplastic Syndromes (MDS)[1].
PD-1-IN-17 is a programmed cell death- 1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM[1].
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3].
Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM[1].
Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally active AHR agonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety[1][2][3].
P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease[1].
Urabrelimab (SRF231) is a fully human anti-CD47 monoclonal antibody that blocks the CD47-SIRP interaction[1].
Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury[1][2][3].
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
Usnoflast is a NLRP3 modulator, as well as a non-steroidal anti-inflammatory agent (NSAD)[1].
4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine has the potential for the research of immune-related diseases such as cancer and autoimmune disorders[1][2].
BEC HCl is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM (ph 7.5).target: Arginase II [1];In vitro: BEC HCl causes significant enhancement of NO-dependent smooth muscle relaxation in this tissue. [2] BEC HCl enhances perivascular and peribronchiolar lung inflammation, mucus metaplasia, NF-κB DNA binding, and mRNA expression of the NF-κB-driven chemokine genes CCL20 and KC, and lead to further increases in airways hyperresponsiveness. [3] In vivo: BEC HCl increased contractility in isolated myocytes from WT and NOS3 but not NOS1 knockout mice. [4]
IONIS-FB-LRx is a specific antisense oligonucleotide (ASO) targeting complement factor B (CFB). IONIS-FB-LRx effectively reduces circulating levels of CFB. IONIS-FB-LRx can be used for geographic atrophy (GA) research[1][2].
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells[1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells[2].
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis[1][2][3].
Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity[1].
Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research[1][2].
MLN 3897 is a potent, specific and orally active antagonist of CCR1 with IC50 of 0.8 nM in competition binding assays, 500-fold selectivity over CCR5; inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-fos signaling, inhibits osteoclastogenesis and OC activity by impairing multinucleation and by down-regulation of c-Fos signaling; demonstrates potential for the treatment of multiple sclerosis and rheumatoid arthritis. Multiple Sclerosis Phase 1 Discontinued
COX-1/2-IN-3 (Compound 7a) is a COX-1 and COX-2 inhibitor. COX-2-IN-15 shows anti-inflammatory activity with low toxicity[1].
Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].
Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and an IL-2 variant that only binds IL-2Rβγ. Isotype: human IgG1[1].
COX-2-IN-23 (compound 9a) is a selective COX-2 inhibitor with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1. COX-2-IN-23 has anti-inflammatory activity and low ulcerogenic activity.
Carboxy-PTIO is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model[1][2][3].
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders[1].
E7766 diammonium salt is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 diammonium salt shows potent pan-genotypic and antitumor activities[1].