Farnesyl Transferase

Farnesyl Transferase(法尼基转移酶)

Farnesyltransferase is one of the three enzymes in the prenyltransferase group. Farnesyltransferase's targets include members of the Ras superfamily of small GTP-binding proteins critical to cell cycle progression.

Farnesyltransferase inhibitors (FTIs) are small-molecule inhibitors that selectively inhibit farnesylation of a number of intracellular substrate proteins such as Ras. Farnesyl transferase inhibitors (FTIs) represent a new class of signaling inhibitors that is emerging in the clinical arena of hematologic malignancies and that may inhibit critical growth and survival signals. FTIs are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in cancer.

Farnesyl Transferase 相关产品(20)

  • GC10265 structure
    GC10265Manumycin A
    CAS: 52665-74-4
    纯度: >98.00%

    A farnesyltransferase inhibitor with antitumor activity

  • GC10330 structure
    GC10330Lonafarnib
    CAS: 193275-84-2
    纯度: >98.50%

    A farnesyltransferase inhibitor with antitumor activity

  • GC15442 structure
    GC15442Tipifarnib (Zarnestra)
    CAS: 192185-72-1
    纯度: >98.50%

    A farnesyltransferase inhibitor with antitumor activity

  • GC16310 structure
    GC16310FTI 277 HCl
    CAS: 180977-34-8
    纯度: >99.00%

    FTI 277 HCl是一种强效且具有选择性的法尼基转移酶(FTase)抑制剂,IC 50 值为0.5nM,较香叶酰基香叶转移酶I(GGTase I)选择性高出约100倍。

  • GC31242 structure
    GC31242LNK754
    CAS: 439153-64-7

    LNK754 是 CP-609754 的外消旋体。

  • GC31276 structure
    GC31276Prenyl-IN-1
    CAS: 360561-53-1

    Prenyl-IN-1是一种prenylation抑制剂,尤其是香叶烯基转移酶(geranylgeranyltransferase)或法尼基转移酶(farnesyltransferase)的抑制剂,在帕金森研究中,具有抗氧化应激作用。

  • GC31516 structure
    GC31516YM-53601 free base
    CAS: 182959-28-0

    A squalene synthase inhibitor

  • GC31556 structure
    GC31556RPR107393 free base
    CAS: 197576-78-6

    RPR107393freebase是一种有效的选择性角鲨烯合酶(squalenesynthase)抑制剂,抑制鼠肝微粒体角鲨烯合成酶,IC50值为0.8±0.2nM。

  • GC32759 structure
    GC32759L-778123 hydrochloride (L-778,123 hydrochloride)
    CAS: 253863-00-2
    纯度: >98.50%

    A dual inhibitor of FTase and GGTase I

  • GC32865 structure
    GC32865BMS-214662
    CAS: 195987-41-8
    纯度: >99.50%

    A potent FTase inhibitor

  • GC33007 structure
    GC33007Tipifarnib S enantiomer ((S)-(-)-R-115777)
    CAS: 192185-71-0

    An inactive enantiomer of tipifarnib

  • GC33367 structure
    GC33367FTI 276
    CAS: 170006-72-1

    FTI-276是有效的proteinfarnesyltransferase(PFT)抑制剂,作用于恶性疟原虫和人类的IC50值分别为0.9和0.5nM。

  • GC36038 structure
    GC36038FGTI-2734
    CAS: 1247018-19-4
    纯度: >99.00%

    FGTI-2734 是 RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT) 抑制剂,对 FT 和 GGT 的 IC50s 分别为 250 nM和 520 nM。 FGTI-2734 可以阻断 KRAS 的膜定位,从而解决 KRAS 耐药性问题,并抑制突变的 KRAS 胰腺肿瘤。

  • GC36086 structure
    GC36086FTI-277
    CAS: 170006-73-2

    FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.

  • GC38807 structure
    GC38807Lapaquistat acetate
    CAS: 189060-13-7
    纯度: >98.00%

    Lapaquistat acetate (TAK-475) 是一种角鲨烯合酶 (squalene synthase) 抑制剂,可阻止法呢基二磷酸酯 (FPP) 转化为角鲨烯。Lapaquistat acetate (TAK-475) 最初旨在用于甲羟戊酸激酶缺乏症 (MKD),可有效降低低密度脂蛋白胆固醇,但可能引起肝脏损害。

  • GC60548 structure
    GC60548ABT-100
    CAS: 450839-40-4
    纯度: >98.00%

    ABT-100是一种有效的,高选择性和口服活性的farnesyltransferase抑制剂。ABT-100抑制细胞增殖(对于EJ-1,DLD-1,MDA-MB-231,HCT-116,MiaPaCa-2,PC-3和DU-145细胞的IC50分别为2.2nM,3.8nM,5.9nM,6.9nM,9.2nM,70nM和818nM),可增加细胞凋亡并减少血管生成。ABT-100具有广谱抗肿瘤活性。

  • GC60861 structure
    GC60861FTI-2153
    CAS: 344900-92-1
    纯度: >99.00%

    FTI-2153是一种有效、高度选择性的法尼基转移酶farnesyltransferase(FTase)抑制剂,IC50为1.4nM。FTI-2153有效抑制H-Ras蛋白的加工修饰,IC50值为10nM,是对其抑制活性是对Rap1A蛋白加工的3000多倍。

  • GC61318 structure
    GC61318Tectol
    CAS: 24449-39-6

    Tectol,从Lippiasidoides中分离,对人白血病细胞株HL60和CEM具有显著的抑制作用。Tectol是一种farnesyltransferase(FTase)抑制剂,在人和布氏锥虫的IC50分别为2.09和1.73μM。Tectol抑制耐药恶性疟原虫(FcB1),IC50为3.44μM。

  • GC61775 structure
    GC61775FTI-2153 TFA
    纯度: >98.00%

    FTI-2153TFA是一种有效、高度选择性的法尼基转移酶farnesyltransferase(FTase)抑制剂,IC50为1.4nM。FTI-2153TFA有效抑制H-Ras蛋白的加工修饰,IC50值为10nM,是对其抑制活性是对Rap1A蛋白加工的3000多倍。

  • GC62276 structure
    GC62276CP-609754
    CAS: 1190094-64-4

    CP-609754 (LNK-754) 是一种有效且可逆的法尼基转移酶(farnesyltransferase) 抑制剂,具有潜在的抗癌活性。CP-609754 抑制重组人 H-Ras 和重组 K-Ras法尼基化的 IC50 分别为 0.57 ng/mL 和 46 ng/mL。