Transferase

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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)
目录号	产品目录	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
S9231	Schisanhenol	-1 mg/mL	81 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	21 mg/mL	21 mg/mL	-1 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
S8608	Adenosine Dialdehyde (ADOX)	3 mg/mL	19 mg/mL	<1 mg/mL
S3945	L-Cycloserine	20 mg/mL	8 mg/mL	-1 mg/mL
S3658	O6-Benzylguanine	<1 mg/mL	48 mg/mL	12 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	Tipifarnib Tipifarnib 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。	Clin Cancer Res, 2012, 18(13):3524-31 J Clin Endocrinol Metab, 2013, 98(6):2502-12 Stem Cells Transl Med, 2014, 3(4):510-9	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.
S2797	Lonafarnib Lonafarnib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。	Antiviral Res, 2017, 141:116-123 J Cell Physiol, 2017, 232(1):192-201 Anticancer Res, 2017, 37(1):149-159	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。	Cancer Discov, 2016, 6(7):727-39 Cancer Lett, 2016, 379(1):1-11 Cell chemical biology, 2018, 10.1016/j.chembiol.2017.12.008	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.
S2674	A922500 A922500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	Lomeguatrib Lomeguatrib是一种有效的O⁶-alkylguanine-DNA-alkyltransferase抑制剂，IC50为5 nM。	Mol Cancer Ther, 2015, 14(5):1236-46 Onco Targets Ther, 2018, 11:3671-3684	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).
S9231^New	Schisanhenol Schisanhenol is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7.
S5336^New	Hecogenin Hecogenin, a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM.
S5449^New	3-Methoxybenzamide 3-Methoxybenzamide is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT).
S4989^New	AOA hemihydrochloride Aminooxyacetic acid是氨基丁酸转氨酶（aminobutyrate aminotransferase）抑制剂，参与氨基酸和聚胺代谢。
S7466	GGTI 298 TFA salt GGTI 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。	Cancer Lett, 2018, 442:40-52. Lymphat Res Biol, 2018, 16(1):43-55 Med Sci Monit, 2018, 24:1484-1492	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	Tolcapone Tolcapone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，K_i为30nM。
S4589	Amodiaquine dihydrochloride dihydrate Amodiaquine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。
S4743	Wogonin Wogonin，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。	Exp Ther Med, 2015, 10(3):1066-1070	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-Cycloserine L-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity.
S3658	O6-Benzylguanine O6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.
S7467	LB42708 LB42708 是一种口服有效的farnesyltransferase (FTase)抑制剂。
S4280	Meclofenoxate (Centrophenoxine) HCl Meclofenoxate (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-04620110 PF-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 HCl FTI 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。	Cancer Lett, 2018, 442:202-212	(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.

研究领域

产品类型

Transferase

信号通路图

研究领域