Transferase
信号通路图
研究领域
抑制剂选择性比较
Transferase产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1453 |
TipifarnibTipifarnib 是一种有效的，特异性farnesyltransferase (FTase)抑制剂，作用于H-ras或N-ras突变细胞，具有最显著的抗增殖作用效果。Phase 3。 |
Effects of tipifarnib on GalN/LPS-induced mortality and ALF in mice. Representative liver histology (H/E staining at 5 h after saline or GalN/LPS) by microscopic images are shown.
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| S2797 |
LonafarnibLonafarnib是一种口服生物有效的FPTase抑制剂，作用于H-ras，K-ras-4B和N-ras，无细胞试验中IC50分别为1.9 nM， 5.2 nM和2.8 nM。Phase 3。 |
Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
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| S2799 |
Daporinad (FK866, APO866)Daporinad (FK866, APO866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase)，无细胞试验中IC50为0.09 nM。Phase 1/2。 |
Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.
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| S2674 |
A922500A922500是人类和小鼠DGAT-1抑制剂，IC50分别为7 nM和24 nM，比作用于相关的酰基转移酶，hERG及抗靶面板的选择性高。 |
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| S8056 |
LomeguatribLomeguatrib是一种有效的O6-alkylguanine-DNA-alkyltransferase抑制剂，IC50为5 nM。 |
Characterization of melanoma cell lines upon MGMT status. A, representative examples of dose-response curves for MGMT+ and MGMT− cells treated with temozolomide (TMZ) with or without lomeguatrib (LOM). Graphs show the average GI50 for temozolomide in the presence or absence of lomeguatrib (B). |
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| S9231New |
SchisanhenolSchisanhenol is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
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| S7466 |
GGTI 298 TFA saltGGTI 298是牛儿基转移酶I（geranylgeranyltransferase I）抑制剂，能够将人类肿瘤细胞细胞周期阻止在G1期并诱导凋亡。 |
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| S8244 |
Etomoxir (Na salt)Etomoxir是不可逆的肉碱棕榈酰基转换酶(CPT-1)的抑制剂，肉碱棕榈酰基转换酶位于线粒体内膜的外侧。 |
Immunoblot analysis of CyclinD1, PCNA, γ-H2AX, cleaved-PRAP and -caspase3 (F) in normal saline or ETO-treated groups were determined at 10 weeks after HFD treatment (n = 10 mice/group).
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| S4021 |
TolcaponeTolcapone是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂，Ki为30nM。 |
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| S4589 |
Amodiaquine dihydrochloride dihydrateAmodiaquine在人红细胞中是一种有效的、非竞争性的组胺N-甲基转移酶抑制剂，其Ki值为18.6 nM。它也被用作抗疟疾药和消炎药。 |
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| S5336 |
HecogeninHecogenin, a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM. |
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| S4743 |
WogoninWogonin，在植物中发现的天然活性黄酮类化合物，是CDK9的抑制剂。在抑制CDK9的浓度下，对CDK2、CDK4和CDK6没有抑制作用。也可抑制N-acetyltransferase。 |
Effect of Wogonin on the translocation and transcriptional activity of NFATc1. U2OS cells stably transfected with EGFP-NFATc1, RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. The IN Cell™ Analyzer 1000 was used to observe the translocation of NFATc1. (A) DMSO was used as a control. RANKL (100 ng/ml) significantly stimulated the translocation of NFATc1; Wogonin (5 mM) significantly decreased the translocation of NFATc1 induced by RANKL (magnification, x200). (B) Statistics showed that Wogonin could decrease the translocation of NFATc1 into the nucleus induced by RANKL in a concentration-dependent manner. RAW264.7 cells were transfected with pGL3-promoter-NFATc1-RE, and then RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. (C) RANKL significantly increased the transcriptional activity of NFATc1 and Wogonin decreased the transcriptional activity of NFATc1 induced by RANKL in a concentration-dependent manner. n=3; *P<0.05 and ***P<0.001 compared with the RANKL group. NAFTc1, nuclear factor of activated T cells c1; EGFP, enhanced green fluorescent protein; DMSO, dimethylsulfoxide, RANKL, receptor activator of nuclear factor κB ligand; RE, response element.
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| S8608 |
Adenosine Dialdehyde (ADOX)Adenosine Dialdehyde (ADOX)是腺苷类似物，同时也是S-adenosylmethionine-dependent methyltransferase抑制剂，IC50为40 nM。 |
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| S3945 |
L-CycloserineL-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity. |
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| S5449 |
3-Methoxybenzamide3-Methoxybenzamide is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT). |
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| S3658 |
O6-BenzylguanineO6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator. |
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| S7467 |
LB42708LB42708 是一种口服有效的farnesyltransferase (FTase)抑制剂。 |
||
| S4989 |
AOA hemihydrochlorideAminooxyacetic acid是氨基丁酸转氨酶（aminobutyrate aminotransferase）抑制剂，参与氨基酸和聚胺代谢。 |
||
| S4280 |
Meclofenoxate (Centrophenoxine) HClMeclofenoxate (Centrophenoxine) HCl 是一种抗衰老药，用于治疗老年痴呆和阿尔茨海默氏病, 同时也可抑制cholinephosphotransferase的活性。 |
||
| S7192 |
PF-04620110PF-04620110是一种口服有效的，选择性甘油二酯酰基转移酶-1(DGAT1)抑制剂，IC50为19 nM。 |
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| S7465 |
FTI 277 HClFTI 277 HCl是FTI 277的甲酯，是一种有效的选择性farnesyltransferase (FTase)抑制剂，IC50为500 pM，选择性比密切相关的GGTase I 高100倍。 |
(A) HCT 116 cells were treated with Tram (0, 30, or 60 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD. (B) SW480 and MDA-MB-231 cells were treated with Tram (0, 80, 160 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1453 |
TipifarnibTipifarnib 是一种有效的，特异性farnesyltransferase (FTase)抑制剂，作用于H-ras或N-ras突变细胞，具有最显著的抗增殖作用效果。Phase 3。 |
Effects of tipifarnib on GalN/LPS-induced mortality and ALF in mice. Representative liver histology (H/E staining at 5 h after saline or GalN/LPS) by microscopic images are shown.
|
|
| S2797 |
LonafarnibLonafarnib是一种口服生物有效的FPTase抑制剂，作用于H-ras，K-ras-4B和N-ras，无细胞试验中IC50分别为1.9 nM， 5.2 nM和2.8 nM。Phase 3。 |
Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
|
|
| S2799 |
Daporinad (FK866, APO866)Daporinad (FK866, APO866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase)，无细胞试验中IC50为0.09 nM。Phase 1/2。 |
Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.
|
|
| S2674 |
A922500A922500是人类和小鼠DGAT-1抑制剂，IC50分别为7 nM和24 nM，比作用于相关的酰基转移酶，hERG及抗靶面板的选择性高。 |
||
| S8056 |
LomeguatribLomeguatrib是一种有效的O6-alkylguanine-DNA-alkyltransferase抑制剂，IC50为5 nM。 |
Characterization of melanoma cell lines upon MGMT status. A, representative examples of dose-response curves for MGMT+ and MGMT− cells treated with temozolomide (TMZ) with or without lomeguatrib (LOM). Graphs show the average GI50 for temozolomide in the presence or absence of lomeguatrib (B). |
|
| S9231New |
SchisanhenolSchisanhenol is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
||
| S7466 |
GGTI 298 TFA saltGGTI 298是牛儿基转移酶I（geranylgeranyltransferase I）抑制剂，能够将人类肿瘤细胞细胞周期阻止在G1期并诱导凋亡。 |
||
| S8244 |
Etomoxir (Na salt)Etomoxir是不可逆的肉碱棕榈酰基转换酶(CPT-1)的抑制剂，肉碱棕榈酰基转换酶位于线粒体内膜的外侧。 |
Immunoblot analysis of CyclinD1, PCNA, γ-H2AX, cleaved-PRAP and -caspase3 (F) in normal saline or ETO-treated groups were determined at 10 weeks after HFD treatment (n = 10 mice/group).
|
|
| S4021 |
TolcaponeTolcapone是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂，Ki为30nM。 |
||
| S4589 |
Amodiaquine dihydrochloride dihydrateAmodiaquine在人红细胞中是一种有效的、非竞争性的组胺N-甲基转移酶抑制剂，其Ki值为18.6 nM。它也被用作抗疟疾药和消炎药。 |
||
| S5336 |
HecogeninHecogenin, a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM. |
||
| S4743 |
WogoninWogonin，在植物中发现的天然活性黄酮类化合物，是CDK9的抑制剂。在抑制CDK9的浓度下，对CDK2、CDK4和CDK6没有抑制作用。也可抑制N-acetyltransferase。 |
Effect of Wogonin on the translocation and transcriptional activity of NFATc1. U2OS cells stably transfected with EGFP-NFATc1, RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. The IN Cell™ Analyzer 1000 was used to observe the translocation of NFATc1. (A) DMSO was used as a control. RANKL (100 ng/ml) significantly stimulated the translocation of NFATc1; Wogonin (5 mM) significantly decreased the translocation of NFATc1 induced by RANKL (magnification, x200). (B) Statistics showed that Wogonin could decrease the translocation of NFATc1 into the nucleus induced by RANKL in a concentration-dependent manner. RAW264.7 cells were transfected with pGL3-promoter-NFATc1-RE, and then RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. (C) RANKL significantly increased the transcriptional activity of NFATc1 and Wogonin decreased the transcriptional activity of NFATc1 induced by RANKL in a concentration-dependent manner. n=3; *P<0.05 and ***P<0.001 compared with the RANKL group. NAFTc1, nuclear factor of activated T cells c1; EGFP, enhanced green fluorescent protein; DMSO, dimethylsulfoxide, RANKL, receptor activator of nuclear factor κB ligand; RE, response element.
|
|
| S8608 |
Adenosine Dialdehyde (ADOX)Adenosine Dialdehyde (ADOX)是腺苷类似物，同时也是S-adenosylmethionine-dependent methyltransferase抑制剂，IC50为40 nM。 |
||
| S3945 |
L-CycloserineL-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity. |
||
| S5449 |
3-Methoxybenzamide3-Methoxybenzamide is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT). |
||
| S3658 |
O6-BenzylguanineO6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator. |
||
| S7467 |
LB42708LB42708 是一种口服有效的farnesyltransferase (FTase)抑制剂。 |
||
| S4989 |
AOA hemihydrochlorideAminooxyacetic acid是氨基丁酸转氨酶（aminobutyrate aminotransferase）抑制剂，参与氨基酸和聚胺代谢。 |
||
| S4280 |
Meclofenoxate (Centrophenoxine) HClMeclofenoxate (Centrophenoxine) HCl 是一种抗衰老药，用于治疗老年痴呆和阿尔茨海默氏病, 同时也可抑制cholinephosphotransferase的活性。 |
||
| S7192 |
PF-04620110PF-04620110是一种口服有效的，选择性甘油二酯酰基转移酶-1(DGAT1)抑制剂，IC50为19 nM。 |
||
| S7465 |
FTI 277 HClFTI 277 HCl是FTI 277的甲酯，是一种有效的选择性farnesyltransferase (FTase)抑制剂，IC50为500 pM，选择性比密切相关的GGTase I 高100倍。 |
(A) HCT 116 cells were treated with Tram (0, 30, or 60 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD. (B) SW480 and MDA-MB-231 cells were treated with Tram (0, 80, 160 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD.
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