N-(4-ベンジルピペラジン-1-イル)-1-(3,5-ジメチル-1-フェニル-1H-ピラゾール-4-イル)メタンイミン 化学特性,用途語,生産方法
外観
白色〜黄色, 結晶〜粉末
溶解性
メタノールに溶ける。
説明
Smoothened (SMO) is a GPCR-
like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC
50 = 20 nM). It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO. SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated. Through antagonism of SMO, SANT 1 represses Gli-
mediated transcription in a variety of cell types.
化学的特性
Pale Yellow Solid
使用
Treatment of Anaplastic lymphoma kinase (ALK)-positive anaplastic large cell lymphoma cells
2 and chronic lymphocytic leukemia cells
3 with SANT-1 induced cell death.
生物活性
Potent, cell-permeable inhibitor of Sonic hedgehog (Shh) signaling; high affinity antagonist of smoothened activity (K D = 1.2 nM). Inhibits smoothened agonist effects with an IC 50 of 20 nM (in Shh-LIGHT2 cells).
N-(4-ベンジルピペラジン-1-イル)-1-(3,5-ジメチル-1-フェニル-1H-ピラゾール-4-イル)メタンイミン 上流と下流の製品情報
原材料
準備製品