FTase inhibitor I is a potent inhibitor of farnesyltransferase (FTase; IC = 21 nM) that is greater than 30-fold selective for FTase over geranylgeranyl transferase (GGTase; IC = 790 nM). It prevents farnesylation of Ras and inhibits proliferation of cells transformed by Ras farnesylation. In a dog model of subarachnoid hemorrhage, it reduces GTP-Ras in spastic basilar arteries, decreases angiographic vasospasm, and improves clinical scores.
Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras).
体外研究
Ftase inhibitor I (B581) inhibits the ability of only Ras-F-transformed cells, but not geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras)- (or Raf-) transformed cells, to grow in soft agar.
分子式
C22H38N4O3S2
分子量
470.7
CAS号
149759-96-6
中文名称
N-[(2S)-((2R)-2-氨基-3-巯基丙基氨基)-3-甲基丁基]-L-苯丙氨酰-L-蛋氨酸
运输条件
Room temperature in continental US; may vary elsewhere.