Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13069 |
Talabostat isomer mesylate
|
Others | Others |
Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available inhibitor of dipeptidyl peptidase IV (DPP-IV)(Ki of 0.18 nM). | |||
T4042 |
Talabostat mesylate
Val-boroPro,PT100 |
Proteasome; DPP-4 | Proteases/Proteasome; Ubiquitination |
Talabostat mesylate (PT100) 是一种具有口服活性和非选择性的二肽基肽酶 IV 抑制剂(IC50< 4 nM;Ki= 0.18 nM)。Talabostat mesylate 是成纤维细胞活化蛋白的第一个临床抑制剂(IC50= 560 nM),抑制 DPP8/9 (IC50= 4/11 nM;Ki= 1.5/0.76 nM),静息细胞脯氨酸二肽酶(IC50= 310 nM)、DPP2 和一些其他 DASH 家族酶。Talabostat mesylate 具有抗肿瘤和造血刺激活性 。 | |||
T37861 |
Talabostat
|
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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,... |