as 183

AS 183 is an inhibitor of cholesterol acyltransferase (ACAT).

SSJ-183 is a low-toxicity and orally available and anti-malarial drug with an IC50 = 7.6 nM against P. falciparum and no lethality at doses up to 2000 mg/kg po.

Poloxamer 183 L63 is a block copolymer of polyoxyethylene and polyoxypropylene, with an average molecular weight of 2000. It demonstrates antibacterial activity by inhibiting 83% of Mycobacterium avium at a concentration of 1 mg/mL. Poloxamer 183 L63 can form thermoreversible hydrogels and is used as a food additive, as well as a drug delivery carrier in cosmetics, pharmaceuticals, and tissue engineering.

SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.

CRBN ligand-183 is a CRBN-type E3 ubiquitin ligase ligand, used in the preparation of PROTAC.

E3LigaseLigand-linker Conjugate 183 is an E3 ligase ligand-linker conjugate of PCSK9 autophagy degrader 2. It comprises the LC3B ligand 2 and its corresponding linker.

GPR183 antagonist-3 (compound 33) is an orally active GPR183 antagonist with an IC50 value of 8.7 μM. It demonstrates significant in vitro anti-migration and anti-inflammatory activity in monocytes and can alleviate pathological symptoms in experimental colitis induced by dextran sulfate sodium.

GPR183 inverse agonist-1 (Compound 78) is an inverse agonist of GPR183. It inhibits GPR183-mediated Gi activation and β-arrestin2 recruitment while blocking PBMC migration. This compound is utilized in research concerning inflammation, autoimmune, and cancer-related diseases.

Anticancer agent 183 (compound 4h) exhibits potent inhibition of matrix metalloproteinase-9 (MMP-9), reducing its viability by more than 75% at a concentration of 100 μg/mL. Additionally, it demonstrates significant anticancer activity, with an IC50 value of <0.14 μM against the A549 cell line and induces apoptotic [1] processes.

GPR183 antagonist-2 (compound 32), a selective antagonist of GPR183, exhibits excellent water solubility and pharmacokinetic properties. This compound effectively diminishes paw and joint swelling, and reduces gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a dose-dependent manner within a collagen-induced arthritis (CIA) mouse model. GPR183 antagonist-2 is applicable in researching autoimmune diseases [1].

GPR183-IN-2 (compound 23) is an effective, orally active inhibitor of GPR183, displaying an IC50 value of 39.45 nM in Ca2+ mobilization assays. This compound has potential applications in research related to cancer, autoimmune diseases, pain, and osteoporosis.

GPR183-IN-1 (compound 15) is an effective orally active inhibitor of GPR183. It inhibits Ca2+ mobilization with an IC50 value of 39.97 nM. GPR183-IN-1 holds potential for research in cancer, autoimmune diseases, pain, and osteoporosis.

The compound, Anti-CXCR3/GPR9/CD183 Antibody, is a humanized antibody expressed in CHO, targeting CXCR3/GPR9/CD183. It features huIgG1 heavy chains and huκ light chains, with a predicted molecular weight (MW) of 150 kDa. For isotype control, please refer to HumanIgG1kappa, Isotype Control.

The Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173) is an IgG antibody inhibitor derived from a hamster originating from the United States, specifically targeting mouse CXCR3/CD183.

TCS 183 can mimic the Akt phosphorylation site on GSK3β preventing conditioning of LTD.

Leishmania peptide 183 is an antigen.

PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor with an IC50 of 1.8 nM, demonstrating antitumor activity [1].

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to be determined. 1.Serhan, C.N., Gotlinger, K., Hong, S., et al.Anti-inflammatory actions of neuroprotectin D1/protectin D1 and its natural stereoisomers: Assignments of dihydroxy-containing docosatrienesJ. Immunol.176(3)1848-1859(2006) 2.Ariel, A., and Serhan, C.N.Resolvins and protectins in the termination program of acute inflammationTRENDS in Immunology28(4)176-183(2007) 3.Schwab, J.M., Chiang, N., Arita, M., et al.Resolvin E1 and protectin D1 activate inflammation-resolution programmesNature447(7146)869-874(2007)

Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2 |1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): Role of the alpha-1L adrenoceptor in tissue selectivity, part II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997).