an-168

BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophrenia, Alzheimer's disease, and bi-directional cognitive impairment.

(R)-ADX-47273 is a potent positive allosteric modulator of mGluR5, with an EC50 of 168 nM for potentiation.

ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement

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)

O-Benzylhydroxylamine is a building block.1,2It has been used in the synthesis of β-lactam inhibitor precursors and fluoroquinolone derivatives with antibiotic activity. 1.Bellettini, J.R., and Miller, M.J.A short synthesis of an important precursor to a new class of bicyclic β-lactamase inhibitorsTetrahedron Lett.38(2)167-168(1997) 2.Asadipour, A., Moshafi, M.H., Khosravani, L., et al.N-substituted piperazinyl sarafloxacin derivatives: synthesis and in vitro antibacterial evaluationDaru.26(2)199-207(2018)

Vulolisib is an orally active and potent inhibitor of phosphatidylinositol 3 kinase (PI3K), acting on PI3Kα (IC50: 0.2 nM), PI3Kβ (IC50: 168 nM), PI3Kγ (IC50: 90 nM), PI3Kδ (IC50: 49 nM). activity and exhibits anti-proliferative activity against cancer cells.

Neihulizumab (ALTB-168), an immune checkpoint agonistic antibody, targets and binds to human CD162 (PSGL-1), resulting in the downregulation of activated T-cells. It is utilized in research aimed at treating steroid-refractory acute graft-versus-host disease (SR-aGVHD), psoriasis, psoriatic arthritis, and ulcerative colitis [1].

Compound D16 (Anticancer agent 168) is an inhibitor of DNA2 that induces apoptosis and cell-cycle arrest predominantly in the S-phase. It demonstrates anticancer efficacy and can counteract chemotherapy resistance in cancers harboring mutant p53 [1].

HSD17B13-IN-65 (Compound 168) acts as an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating potent activity with an IC50 value of ≤ 0.1 μM for estradiol. It is applicable in the study of various diseases, including liver, metabolic, and cardiovascular conditions like NAFLD or NASH, and in investigations of drug-induced liver injury (DILI) [1].

Antitumor agent-168 (compound 21b) disrupts the microtubule networks within tumor cells, leading to G2 M cell cycle arrest and induction of apoptosis. It inhibits the growth of MCF-7 cells with an IC50 value of 1.4 nM.

Sublancin is an antimicrobial peptide that inhibits DNA replication, transcription, and translation without affecting membrane integrity, and suppresses glucose uptake through competition with the phosphotransferase system (PTS). Sublancin inhibits B. subtilis strain 168 ΔSPβ with a MIC of 0.312 μM [1][2].