az 1

AZ-1 is an inducer of ABCA1 and apoE. It enhances ABCA1 activity and decreases P2X7 receptor activity. AZ-1 activates endogenous LXR signaling but shows no direct LXRα or LXRβ agonist activity.

AZ 11645373 (3-[1-[[(3'-NITRO[1,1'-BIPHENYL]-4-YL)OXY]METHYL]-3-(4-PYRIDINYL)PROPYL]-2,4-THIAZOLIDINEDIONE) is a highly selective and potent human P2X7 receptor antagonist that has no effect on mouse rat P2X7 receptor.

AZ-PRMT5i-1 (Compound 28) is an effective, orally-active MTAP-selective PRMT5 inhibitor. It exhibits synergistic properties with MTA and demonstrates anti-tumor activity both in vivo and in vitro, making it suitable for research in cancers lacking MTAP.

FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999

AZ 14145845, a potent and highly selective dual Mer Axl kinase inhibitor (pIC50 = 7 nM and 7.8 nM in pAxl and pMer, respectively), demonstrates significant efficacy in reducing tumor growth in a dose-dependent manner within the Mer and Axl kinase Ba F3 tumor xenograft model in vivo. When combined with anti-PD1 antibodies and ionizing radiation, this compound enhances survival rates in mice bearing MC38-derived tumors. Additionally, AZ 14145845 is orally bioavailable.

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

AZ PFKFB3 26 is an effective and selective PFKFB3 inhibitor with an IC50 of 23 nM. The IC50s for PFKFB1 and PFKFB2 are 2.06 and 0.384 μM, respectively.

LpxH-IN-AZ1 is a potent inhibitor of the UDP-2,3-diacylglucosamine pyrophosphate hydrolase, LpxH, and sulfonylpiperazine compounds.LpxH-IN-AZ1 exhibits antimicrobial activity and inhibits Klebsiella pneumoniae with an IC50 of 0.36 μM.

AzddMeC (Az-Dcme) is a nucleoside analog with antiviral activity and is an orally active and selective inhibitor of HIV-1 reverse transcriptase and HIV-1 replication.AzddMeC has an EC50 value of 9 nM against HIV-1-infected human PBM cells and 6 nM against HIV-1-infected human macrophages.

AZ3976 is an inhibitor of PAI-1 with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 displays profibrinolytic activities.

TBA-7371 (DprE1-IN-1) is a potent inhibitor of DprE1 and PDE6.

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

AZ-GHS-22 is an inverse agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor.1It binds to GHS-R1a with an IC50value of 0.77 nM. AZ-GHS-22 decreases food intake in mice by 54% in the first two hours after administration of a 100 mg/kg dose. 1.McCoull, W., Barton, P., Brown, A.J.H., et al.Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonistsJ. Med. Chem.57(14)6128-6140(2014)

AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

Naloxegol (NKTR-118; AZ-13337019) is an opioid receptor antagonist[1].

AZ5104 is a potent EGFR inhibitor.

AZ'6421, functioning as a Proteolysis Targeting Chimera (PROTAC), selectively degrades estrogen receptor alpha, demonstrating potent anti-tumor activity by inhibiting uncontrolled cellular proliferation characteristic of malignant diseases. This compound holds promise for cancer research, including breast cancer applications [1].

AZ7550 hydrochloride (AZ7550 hydrochloride ), an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

USP25 28 inhibitor AZ1 is a selective, orally active and non-competitive dual ubiquitin-specific protease USP25 28 inhibitor with IC50 of 0.7 μM and 0.6 μM, respectively, and exhibits anti-inflammatory and anti-tumor effects.

AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with an IC50=11nM for PFKFB3, reduces MCL-1, and inhibits angiogenesis by decreasing lactic acid production and ATP levels in endothelial cells (ECs) in tube-forming assays, and has neuroprotective effects.

AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.