Transferase
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1453 | Tipifarnib | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S2797 | Lonafarnib | <1 mg/mL | 127 mg/mL | 127 mg/mL |
| S2799 | Daporinad (FK866, APO866) | <1 mg/mL | <1 mg/mL | 78 mg/mL |
| S2674 | A922500 | <1 mg/mL | 86 mg/mL | <1 mg/mL |
| S8056 | Lomeguatrib | <1 mg/mL | 65 mg/mL | <1 mg/mL |
| S5336 | Hecogenin | <1 mg/mL | <1 mg/mL | <1 mg/mL |
| S5449 | 3-Methoxybenzamide | -1 mg/mL | 30 mg/mL | -1 mg/mL |
| S4989 | AOA hemihydrochloride | -1 mg/mL | 21 mg/mL | -1 mg/mL |
| S3945 | L-Cycloserine | 20 mg/mL | 8 mg/mL | -1 mg/mL |
| S8608 | Adenosine Dialdehyde (ADOX) | 3 mg/mL | 19 mg/mL | <1 mg/mL |
| S3658 | O6-Benzylguanine | <1 mg/mL | 48 mg/mL | 12 mg/mL |
| S7466 | GGTI 298 TFA salt | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8244 | Etomoxir (Na salt) | 64 mg/mL | 64 mg/mL | 13 mg/mL |
| S4021 | Tolcapone | <1 mg/mL | 55 mg/mL | 55 mg/mL |
| S4589 | Amodiaquine dihydrochloride dihydrate | 29 mg/mL | 92 mg/mL | <1 mg/mL |
| S4743 | Wogonin | <1 mg/mL | 56 mg/mL | 3 mg/mL |
| S7467 | LB42708 | <1 mg/mL | 100 mg/mL | 86 mg/mL |
| S4280 | Meclofenoxate (Centrophenoxine) HCl | 58 mg/mL | 58 mg/mL | 58 mg/mL |
| S7192 | PF-04620110 | <1 mg/mL | 49 mg/mL | <1 mg/mL |
| S7465 | FTI 277 HCl | 17 mg/mL | 96 mg/mL | 14 mg/mL |
- Transferase抑制剂（21）
- 新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。 |
Effect of the inhibition of mutated RAS on thyroid cancer cell response to gefitinib . C-643 (RAS mutated thyroid cancer cells) and BC-PAP (wild type RAS thyroid cancer cells) were seeded in 96-well plates and incubated with increasing doses of gefitinib (Gef.; 0.5, 1.0 , and 5.0 uM), the RAS inhibitor tipifarnib (0.1, 1.0 and 10 uM) or both for 48 hours. Cell viability was then measured by the MTT assay.
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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。 |
Bar graph showing the effect of the PBEF inhibitor FK866 on PLB-induced autophagy in PC-3 cells. Data are presented as the mean ± SD of three independent experiments. *P<0.05; **P<0.01; and ***P<0.001 by one-way ANOVA.
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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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| S5336New |
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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| S5449New |
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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| S4989New |
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。 |
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| S3945New |
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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| S8608New |
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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| S3658New |
O6-BenzylguanineO6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator. |
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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。 |
CPT1A inhibitor counteracted the protective effect of BBR against PA-induced lipid accumulation and apoptosis in HK-2 cells. HK-2 cells were pretreated with or without 40 μmol/L Etomoxir for 24 h, and then treated with 12.5 μmol/L BBR in the presence or absence of 450 μmol/L PA for 24 h. Intracellular lipid content was detected by Oil Red O staining (400×) (A) .
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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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| 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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| S7467 |
LB42708LB42708 是一种口服有效的farnesyltransferase (FTase)抑制剂。 |
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| 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。 |
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| 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。 |
