az-3

AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).

FAZ-3780 (compound G3Ib) is an inhibitor that binds to the NTF2L domain of G3BP1/2, exhibiting a binding affinity to G3BP1 with a Kd of 0.54 μM. It specifically targets the protein-protein interaction domain of G3BP1/2 and inhibits the co-condensation of G3BP1, caprin 1, and RNA in vitro.

FAZ-3532 is a potent G3BP inhibitor that binds to G3BP1 with a dissociation constant (Kd) of 0.54 μM, inhibiting the co-condensation of G3BP1, Caprin1, and RNA, and preventing the formation of intracellular stress granules. It selectively targets the protein-protein interactions within the G3BP1 NTF2L domain without affecting its dimerization or RNA binding, making it an effective tool for studying the immunological role of stress granules during viral infections.

AZ31 is an ATM inhibitor with potency, high selectivity, and oral activity.AZ31 inhibits ATM enzymes, intracellular ATM, with IC50 values of <1.2 nM and 46 nM, respectively.AZ31 exhibits excellent ATR selectivity, PIKK family selectivity, and pan-kinase selectivity.AZ31 is a potent in vitro radiosensitizer that can be used for cancer research.

AZ3246 is an orally active, selective inhibitor of HPK1 with an IC50 of less than 3 nM. It induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 also functions as a low-volume, low-clearance antitumor compound.

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

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

LDHA-IN-4 (AZ33) is an LDHA inhibitor. Binding affinity to 6-His-tagged human LDHA (2 to 322 amino acid residue) expressed in Escherichia coli BL21 (DE3) cells by SPR analysis with an active value of 0.093 μM.

AZ32 is an orally bioavailable, blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for the ATM enzyme and an IC50 of 0.31 μM for ATM in cells.

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, effectively inhibiting BRAF (WT), BRAF (V600E), and wild-type CRAF [IC50s: 79/38/68 nM].

AZ3391 is a quinoxaline derivative that is a potent inhibitor of PARP. AZ3391 has potential for the study of diseases and conditions occurring in central nervous system tissues (e.g., brain and spinal cord).

GCC-4401C methanesulfonate is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).

AZ3971 is a potent BACE1 inhibitor. AZ3971 blocks BACE1-mediated cleavage of APP and inhibits Aβ42 production HEK cells overexpressing the APP protein which carries the Swedish mutation (HEK.APPswe).

AZ'3137 (Compound 22) is an orally active PROTAC-based androgen receptor (AR) degrader, exhibiting a DC50 value of 22 nM. It inhibits cell proliferation in LNCaP cells with a GI50 of 74 nM. Additionally, AZ'3137 suppresses AR signaling and tumor growth in a prostate cancer mouse model.

AZ3451 is an allosteric antagonist of protease-activated receptor-2 (PAR2, IC50: 23 nM).

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.

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-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.

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.

AZ 5704 (compound 74) is a selective and orally active ATM inhibitor (IC50 = 0.6 nM), which can enhance the anti-tumor activity of irinotecan in the SW620 xenograft model.