murine

Moloney murine leukemia virus reverse transcriptase (MMLV RT) is a monomeric replicative polymerase intrinsic to the retrovirus life cycle [1].

Tetrahydrozoline hydrochloride (Murine Plus) is an imidazoline derivative with alpha receptor agonist activity.

Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.

Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.

Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4). Cl-amidine hydrochloride induces apoptosis in cancer cells and it also induces microRNA (miR)-16 in vitro causing cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation. It improves survival in a murine sepsis model.

Avacopan (CCX168) is an orally administered small-molecule C5aR ( IC50 : 0.1 nM.)antagonist that blocks the effects of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a murine model of AAV.

KX2-361 is a orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma

17α-Hydroxyprogesterone acetate possesses progestational activity. 17α-Hydroxyprogesterone acetate shows antiinflammatory effects at the murine maternal-fetal interface.

Iα52 acetate is a naturally processed peptide encompassed the residues 52-68 of the murine I-Eα chain and may contribute to selection of immature T cells.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

JI130 is able to impair the ability of Hes1 to repress transcription. JI130 treatment significantly reduced tumor volume in a murine pancreatic tumor xenograft model.

Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

KYN-101 is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.

Radioprotectin-1 is a selective agonist of LPA2 with EC50 of 25 nM for murine LPA2 GPCR and exerts radioprotective and radiomitigative action.

Amurine (C09334) is an alkaloid isolated from P. stylatum with potential antibacterial activity.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

Yoda1 is a Piezo1 ion channel agonist (EC50s = 17.1 and 26.6 μM for murine and human Piezo1-transfected HEK293T cells, respectively)

Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).

Voriconazole (UK-109496) is a triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.

Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

C29 is a novel inhibitor of TLR2/1 and TLR2/6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages.

N-Acetyl-D-cysteine has antioxidant activities and scavenges ROS through the reaction with its thiol group.

Ginsenoside-F3 has immunoenhancing activity by regulating production and gene expression of type 1, type 2 cytokines in murine spleen cells. Ginsenoside-F3 enhances the NF-kappaB DNA binding activity induced by ConA in murine spleen cells (10 μM).

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Bezafibrate (BM15075) is an antilipemic agent that lowers CHOLESTEROL and TRIGLYCERIDES. It decreases LOW-DENSITY LIPOPROTEINS and increases HIGH-DENSITY LIPOPROTEINS.

Sulesomab (IMMU-MN3), an IgG1 class murine monoclonal antibody fragment, targets the Normal Cross-Reactive Antigen-90 found on leukocytes. The compound nonspecifically accumulates at infection sites due to enhanced permeability of capillary membranes [1].

GSK-LSD1, an LSD1 inhibitor, decreases food consumption and body weight while enhancing insulin sensitivity and glycemic regulation in murine obesity models. Additionally, it mitigates non-alcoholic fatty liver disease (NAFLD) and suppresses cytokine release induced by SARS-CoV-2 in COVID-19 peripheral blood mononuclear cells (PBMCs). Furthermore, GSK-LSD1 inhibits the proliferation and spread of cancer [1] [2] [3].

Eramkafusp alfa is a human IgG1 antibody that targets the murine B lymphocyte antigen CD20, also known as MS4A1 [1].

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and alleviating cognitive deficits in murine schizophrenia models, indicating its potential in antischizophrenia drug research [1].

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg/kg. Nitisinone (3 mg/kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (FAH) deficiency in mice when administered to pregnant dams.2It exhibits hepatoprotective effects inFAH-/-mice, such as prevention of increases in plasma levels of aspartate serine aminotransferase (AST) and conjugated bilirubin, when administration is continued following birth at a dose of 1 mg/kg. Nitisinone (100 μg) decreases urinary excretion of homogentisate and increases urinary excretion of HPPA, HPLA, and 4-hydroxyphenylacetate in a mouse model of alkaptonuria induced by ethylnitrosourea.3Formulations containing nitisinone have been used in the treatment of hereditary tyrosinemia type 1 (HT-1). 1.Ellis, M.K., Whitfield, A.C., Gowans, L.A., et al.Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dioneToxicol. Appl. Pharmacol.133(1)12-19(1995) 2.Grompe, M., Lindstedt, S., al-Dhalimy, M., et al.Pharmacological correction of neonatal lethal hepatic dysfunction in a murine model of hereditary tyrosinaemia type INat. Genet.10(4)453-460(1995) 3.Suzuki, Y., Oda, K., Yoshikawa, Y., et al.A novel therapeutic trial of homogentisic aciduria in a murine model of alkaptonuriaJ. Hum. Genet.44(2)79-84(1999)

ODN 1826, a class B CpG ODN (oligodeoxynucleotide), serves as a potent immunostimulator and a TLR9 agonist in murine models, effectively inducing NO and iNOS production and enhancing cell apoptosis. The sequence for ODN 1826 is 5’-tccatgacgttcctgacgtt-3’ [1] [2] [3].

β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. It is produced via piomelanocortin cleavage in the pituitary gland, hypothalamus, and in lymphocytes, then migrates to its sites of action which include plasma, gut, skin, placenta, cerebrospinal fluid, and cardiac tissues. β-EP induces concentration-dependent decreases in electrically stimulated contraction of the mouse vas deferens that can be reversed by the μ-opioid antagonist CTP and δ-opioid antagonist ICI 174,864. In vivo, β-EP (5 μg, i.c.v.) slows gastrointestinal transit in mice. β-EP (0.5 or 5 μg, i.c.v.) stimulates food intake in rats for 4 to 6 hours, however, this effect is not prolonged with continuous infusion. It antagonizes the appetite-suppressive effects of α-melanocyte-stimulating hormone (α-MSH) for the first three days post administration. β-EP also reduces paralytic demyelination induced by the murine coronavirus MHV-JHM in immunocompetent, but not irradiated or immune-incompetent, mice and rats.

Protectin D1 (also known as neuroprotectin D1 when produced in neuronal tissues) is a DHA-derived dihydroxy fatty acid that exhibits potent protective and anti-inflammatory activities. 10(S),17(S)-DiHDHA is a DHA metabolite, also referred to as protectin DX (PDX). It is produced by an apparent double lipoxygenase (LO)-mediated reaction in murine peritonitis exudates, in suspensions of human leukocytes, or by soybean 15-LO incubated with DHA. It differs from protectin D1 with respect to the stereochemistry of the C-10 hydroxyl and the double bond configuration at the 13 and 15 positions. 10(S),17(S)-DiHDHA blocks neutrophil infiltration in murine peritonitis by 20-25% at a dose of 1 ng/mouse. It also inhibits platelet activation by both impairing thromboxane (TX) synthesis and TX receptor activation.

Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg/mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase/CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto\5′\nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)

Flunixin meglumine (Banamine) is an effective inhibitor of the enzyme cyclooxygenase with anti-inflammatory and antipyretic activity.

MRT-10 is a Smoothened (Smo) receptor antagonist.

Remdesivir de(ethylbutyl 2-aminopropanoate) is a recognized impurity in Remdesivir, a nucleoside analog demonstrating potent antiviral efficacy. It exhibits EC50 values of 74 nM against SARS-CoV and MERS-CoV in human airway epithelial (HAE) cells, and 30 nM against murine hepatitis virus in delayed brain tumor cells. Notably effective in vitro against SARS-CoV-2 (COVID-19) infection, Remdesivir has garnered attention for its application in controlling the spread of the virus, as supported by references [1] [2].

(-)-Chimonanthine (IC50 = 0.93 μM) shows potent inhibitory effects on melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells.

Dafsolimab (SPV-T3a), an IgG2a murine monoclonal antibody (anti-CD3), induces cell death by modulating and activating the CD3/T cell receptor complex and is utilized in research pertaining to graft-versus-host disease (GVHD) [1].

FN-A208 is an active peptide combining A208 from murine laminin a1 with the fibronectin active site GRGDS, linked by a glycine spacer. This compound self-assembles into amyloid-like fibrils and facilitates fibroblast cell adhesion through actin stress fiber formation, suggesting its use as a bioadhesive in tissue regeneration and engineering. FN-A208 targets IKVAV receptors and integrins, but its function can be inhibited by EDTA.

DosatiLink-2 is an inhibitor of the Abelson murine leukemia (ABL) enzyme [1].

Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.

Zarzissine exhibits cytotoxicity against three human and murine tumor cell lines.

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.

Abagovomab (Anti-Human CA-125 Recombinant Antibody) is a murine monoclonal antibody that targets the tumor-associated antigen CA-125. Abagovomab is produced by hybridoma cells in mice. Abagovomab can be used to study ovarian cancer.

1,2,3-Trieicosapentaenoyl-rac-glycerol (EPA-TG) is a glycerol ester of eicosapentaenoic acid , which is an ω-3 fatty acid. An EPA-TG emulsion, administered i.v., lowers leukotriene B4 production by 40% in polymorphonuclear leukocytes from rabbits and reduces platelet aggregation. It suppresses natural killer cell activity both in vitro and in vivo, in human lymphocytes and murine spleens, respectively, with the in vivo effects lasting up to seven days.

Asebotin shows anti-influenza A virus activity, it also possesses potent antiviral activity (100% inhibition at the concentration of 1 ug /mL) against highly pathogenic avian influenza strain H5N1. Asebotin can inhibit the proliferation of murine B cells.

Nagilactone C and phyllanthoside are novel protein synthesis inhibitors, they are specific for the eukaryotic translation apparatus, function in vivo and in vitro, and interfere with translation elongation. Nagilactone C shows high insecticidal activity against second-instar nymphs of Eocanthecona furcellata. Nagilactone C possesses potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines exhibiting ED50 values of 2.3 and 1.2 microg/ml, respectively.

3,3'-Di-O-methylellagic acid reveals moderate antibacterial activity, it also shows strong DPPH radical scavenging activities with SC50 of 123.3 ug/mL. It has a lower capacity of stimulating murine peritoneal macrophages to release nitric oxide and tumoural-alpha necrose factor