T62135
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Tubulin polymerization-IN-25 是一种选择性的、双重 tubulin polymerization (IC50: 1.11 μM) 和 farnesyl transferase (FTase) (IC50: 0.39 μM) 抑制剂。Tubulin polymerization-IN-25 对癌细胞表现出细胞毒性,能够阻断细胞增殖。 |
T15353
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Others
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FTI-2153 is a potent and highly selective farnesyltransferase (FTase) inhibitor (IC50: 1.4 nM). FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. |
T16011
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Prostaglandin Receptor
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Manumycin A is an antibiotic. Manumycin A induces apoptosis and exerts antitumor activity. Manumycin A inhibits exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A acts as a selective, competitive inhibitor of |
T62675
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FTI-277 是一种法尼基转移酶 FTase 抑制剂,也是一种高效 Ras CAAX 肽模拟物。FTI-277 对 H-Ras 和 K-Ras 信号转导具有抑制作用,能够抑制 hepatitis delta virus (HDV) 感染。 |
T64101
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FTI-2153 TFA 是一种高选择性的、有效的法尼基转移酶 farnesyltransferase (FTase) 抑制剂 (IC50: 1.4 nM)。FTI-2153 TFA 可有效抑制 H-Ras 蛋白的加工修饰 (IC50: 10 nM),对其抑制活性是对 Rap1A 蛋白加工的 3000 多倍。 |
T72707
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(Rac)-Lonafarnib (Sch66336外消旋体) 作为Lonafarnib的外消旋体,属于一种口服有效的法尼基蛋白转移酶 (FPTase) 抑制剂,针对H-ras、K-ras及N-ras展现出杰出的抑制效能,其IC50值分别为1.9 nM、5.2 nM和2.8 nM。此外,Lonafarnib还显示出对抗肝炎三角洲病毒 (HDV) 的潜在活性。 |
T69403
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AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma. |
T62844
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GGTI-2154 hydrochloride 是一种有效的、选择性的 geranylgeranyltransferase I (GGTase I) 抑制剂 (IC50: 21 nM)。GGTI-2154 hydrochloride 对 GGTase I 的选择性是 FTase (IC50: 5600 nM) 的 200 倍以上。GGTI-2154 hydrochloride 能够用于研究癌症。 |
T10567
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Raf
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BMS-214662是一种有效的、有选择性的 farnesyl transferase 抑制剂,可诱导原始CD34+慢性髓性白血病(CML)干细胞/祖细胞的线粒体凋亡,具有选择性靶向CML 干细胞/祖细胞的能力,具有抗肿瘤活性。 |