35
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8548 |
Metoprine
|
Histone Methyltransferase; Antifolate; Histamine Receptor | Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Metoprine 是一种有效的组胺 N-甲基转移酶抑制剂,具有抗肿瘤活性。它是一种二氨基嘧啶衍生物,可以透过血脑屏障,并通过抑制 HMT 增加脑组胺水平。 | |||
T8381 |
Amodiaquine
|
Others; Histone Methyltransferase; Parasite | Chromatin/Epigenetic; Microbiology/Virology; Others |
Amodiaquine 是一种合成的4-氨基喹啉类抗疟剂,是一种有口服活性的组胺 N-甲基转移酶抑制剂。它也是一种Nurr1激动剂,有抗炎活性,可特异性结合Nurr1的配体结合域,EC50约为20 μM。 | |||
T2038 |
RG108
N-Phthalyl-L-tryptophan |
DNA Methyltransferase | Chromatin/Epigenetic |
RG108 (N-Phthalyl-L-tryptophan) 是一种非核苷的 DNA 甲基转移酶 (DNMTs) 抑制剂,IC50为115 nM。它阻断 DNA 甲基转移酶的活性位点,可引起抑癌基因的去甲基化和再激活。 | |||
T7157 |
XY1
N-2-萘基-N'-[2-氧代-2-(1-吡咯烷基)乙基]脲 |
Histone Methyltransferase | Chromatin/Epigenetic |
XY1是 SGC707的类似物,SGC707是选择性PRMT3抑制剂,IC50值为31 nM。 | |||
T2352 |
AMI-1
|
Histone Methyltransferase | Chromatin/Epigenetic |
AMI1 是一种有效的、可逆的、细胞渗透性的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂,对人 PRMT1 和酵母 Hmt1p 作用的 IC50值分别为 8.8 和 3.0 μM。它通过阻断肽-底物结合对 PRMTs 发挥抑制作用。 | |||
T0381 |
Amodiaquine dihydrochloride dihydrate
Amodiaquine hydrochloride,阿莫地喹盐酸盐,Amodiaquin dihydrochloride dihydrate |
Histone Methyltransferase; Parasite; Histamine Receptor | Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) 是一种具有口服活性的组胺 N-甲基转移酶抑制剂,也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM。它是 4-氨基喹啉衍生物,具有抗疟和抗炎特性。 | |||
T22956 |
LY 78335
1-(2,3-Dichlorophenyl)ethanamine hydrochloride |
Others | Others |
LY 78335 (1-(2,3-Dichlorophenyl)ethanamine hydrochloride) 是一种苯乙醇胺-N-甲基转移酶 (PNMT) 抑制剂。 | |||
T10363 |
Arazine
N-Acetyl-S-farnesyl-L-cysteine |
Others | Others |
Arazine (N-Acetyl-S-farnesyl-L-cysteine) 可以成为异戊二烯基半胱氨酸甲基转移酶的底物通过与异戊二烯化 G 蛋白或其受体位点竞争。 Arazine 是 G 蛋白和 GPCR 信号传导的细胞渗透性调节剂。 | |||
T7697 |
BIX-01294
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
BIX-01294 是高度选择性的G9a 和GLP 组蛋白甲基转移酶可逆抑制剂。它通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP,可诱导坏死性凋亡和自噬,具有抗肿瘤活性。 | |||
T8106 |
JBSNF-000088
JBSNF000088 |
Others | Others |
JBSNF-000088 是一种烟酰胺的类似物,是一种 NNMT(烟酰胺 N-甲基转移酶) 抑制剂,可作用于人 NNMT (IC50:1.8 µm)、猴 NNMT(IC50:2.8 µm) 和小鼠 NNMT (IC50:5.0 µm)。在代谢性疾病的动物模型中,它能够抑制 NNMT 活性,降低 MNA 水平并驱动胰岛素增敏,调节葡萄糖和减轻体重。 | |||
T8760 |
NNMTi
5-Amino-1-methylquinolinium |
Others | Others |
NNMTi (5-Amino-1-methylquinolinium) 是烟酰胺 N -甲基转移酶的抑制剂 (IC50=1.2 μM),可选择性地结合 NNMT 底物结合位点残基。它能诱导体外成肌细胞分化,提高老年小鼠肌肉干细胞融合和再生能力。 | |||
T1959 |
BIX-01294 trihydrochloride
BIX 01294 |
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
BIX-01294 trihydrochloride 是可逆且高度选择性的G9a 和GLP 组蛋白甲基转移酶抑制剂,IC50分别为 1.9 μM 和 0.7 μM。它可诱导坏死性凋亡和自噬,具有抗肿瘤活性。它通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP。 | |||
T72947 |
JBSNF-000028
JBSNF-000028 free base |
Others | Others |
JBSNF-000028 是一种具有口服活性和有效性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂,对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 具有抑制作用, IC50 分别为 0.033 μM、0.19 μM 和 0.21 μM。JBSNF-000028 可驱动胰岛素敏化、葡萄糖调节和体重减,可用于研究代谢紊乱。 | |||
T27831 |
Lifibrate
|
||
Lifibrate is an inhibitor of cholinephosphotransferase (CPT), phosphatidyl-N,N-dimethylethanolamine N-methyltransferase (PDE-NMT), and phosphatidyl-N-methylethanolamine N-methyltransferase (PME-NMT). | |||
T24604 |
PDAT
Propyl Dimethyl Amino Tryptamine |
||
PDAT is a noncompetitive Indolethylamine N-methyltransferase inhibitor. | |||
T27924 |
LY 87130
LY87130,LY-87130 |
||
LY 87130 is a phenylethanolamine-N-methyltransferase inhibitor. | |||
T71922 | MS2734 | ||
MS2734 is a novel Bisubstrate Inhibitor of Nicotinamide N-Methyltransferase (NNMT). | |||
T27872 |
LY 134046
LY-134046,LY134046,Lilly 134046 |
||
LY 134046 is an inhibitor of phenylethanolamine-N-methyltransferase (PNMT). | |||
T23367 |
SKF 91488 dihydrochloride
|
Others | Others |
histamine N-methyltransferase inhibitor | |||
T68694 |
Quinacrine acetate
|
||
Quinacrine acetate is a histamine N-methyltransferase inhibitor. | |||
T37693 |
N-acetyl-S-geranylgeranyl-L-Cysteine
|
||
N-acetyl-S-geranylgeranyl-L-Cysteine is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins. | |||
T70105 |
Chlorpromazine Sulfone Hydrochloride
|
||
Chlorpromazine Sulfone Hydrochloride is a metabolite of Chlorpromazine -- an anti-emetic and anti-psychotic agent. It may also be used as a potential N-methyltransferase inhibitor. | |||
T36802 |
Bisubstrate Inhibitor 78
|
||
Bisubstrate inhibitor 78 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50= 1.41 μM).1It binds the NNMT active site in the binding pockets for the NNMT substrates S-adenosyl-L-methionine (SAM) and nicotinamide . Bisubstrate inhibitor 78 is selective for NNMT over histone-lysine N-methytransferase NSD2 and protein arginine methyltransferase 1 (PRMT1; IC50s = >50 μM for both). It reduces levels of 1-methylnicotinamide in, and inhibits proliferation of, HSC-2 oral cancer cells when us... | |||
T26744 |
BAY-598 R-isomer
BAY598 R-isomer,BAY 598 R-isomer |
||
BAY-598 R-异构体是BAY589的R-异构体,它可用作参考化合物。它是是赖氨酸N-甲基转移酶(SMYD2)的抑制剂,对SMYD2比蛋白酶激活的受体1(PAR1)具有选择性。 | |||
T83949 |
DC 432
|
||
DC 432是一种强效的N-terminal methyltransferase 1/2 (NTMT1/2) (IC50= 54 nM)肽模拟抑制剂,含有BM30肽和额外五个精氨酸残基。在HCT116细胞中,DC 432处理能够降低调节染色体凝缩1和SET蛋白的N端甲基化水平。该化合物具有细胞渗透性。 | |||
T78163 |
JBSNF-000028 TFA
|
Others | Others |
JBSNF-000028 TFA是一种口服活性烟酰胺N-甲基转移酶(NNMT)抑制剂,其IC50值针对人NNMT (hNNMT)、猴NNMT (mkNNMT) 和小鼠NNMT (mNNMT) 分别为0.033 μM、0.19 μM和0.21 μM。 | |||
T78164 |
JBSNF-000028 hydrochloride
|
Others | Others |
JBSNF-000028 hydrochloride为口服活性烟酰胺N-甲基转移酶(NNMT)抑制剂,对hNNMT、mkNNMT及mNNMT的IC50值分别为0.033 μM、0.19 μM和0.21 μM。 | |||
T28114 |
MS2177
MS 2177,MS-2177 |
||
MS2177 is a potent and selective inhibitor of SETD8, the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). MS2177 has an in vitro IC50 of 1.9 μM (σ = 1.05 μM, n = 4) in ascintillation proximity assay. Binding of MS2 | |||
T22242 | Amodiaquine hydrochloride | ||
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride) 是一种4-氨基喹啉类抗疟剂,是一种有效的口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂,Ki 值为 18.6 nM。Amodiaquine dihydrochloride 也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM,具有抗炎作用。 | |||
T82011 | JBSNF-000028 free base | ||
JBSNF-000028是一种烟酰胺N-甲基转移酶(NNMT)抑制剂,具有口服活性,其针对人类NNMT(hNNMT)、猕猴NNMT(mkNNMT)和小鼠NNMT(mNNMT)的IC50值分别为0.033 μM、0.19 μM和0.21 μM。 | |||
T64189 |
NNMT-IN-3
|
||
NNMT-IN-3 (compound 14) 是一种有效的、选择性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂,在无细胞和基于细胞的实验中的 IC50 值分别为 1.1 nM 和 0.4 μM。NNMT-IN-3 能够用于肥胖、癌症、II 型糖尿病及骨骼肌减少症等疾病的研究。 | |||
T83713 |
DC432 TFA
|
||
DC432是一种细胞内可渗透的肽类抑制剂,针对N-末端Xaa-Pro-Lys N-甲基转移酶1 (NTMT1; IC50 = 0.054 µM)。该化合物与NTMT1和NTMT2有结合作用(Kds分别为0.3和1 µM),并在10和50 µM的浓度下,通过细胞外实验抑制NTMT1对调节染色体凝缩1 (RCC1) N-末端二甲基化。DC432(100 µM)在HCT116细胞中减少了RCC1 SPKRIA基序的三甲基化。 | |||
T81661 |
NNMT-IN-4
|
||
NNMT-IN-4(compound 38),一种选择性、非竞争性且具有膜通透性的烟酰胺N-甲基转移酶(NNMT)抑制剂,在体外生化及细胞实验中的IC50值为42 nM和38 nM。该抑制剂展现出良好的PK/PD关系和安全性,同时具备优秀的口服生物利用度和药物制剂性质,适合作为NNMT活性研究的体内化学探针。 | |||
T81432 | PNMT-IN-1 | ||
PNMT-IN-1(Inhibitor 4)是一种高特异性的PNMT抑制剂,具有1.2 nM的Ki值和81 nM的IC50值。它对DNMT1和DNMT3b也表现出活性,IC50值分别为61 μM和17 μM,并且对肾上腺素具有拮抗效果。PNMT-IN-1属于第二代抑制剂。 | |||
T83867 |
UNC8153 TFA
|
||
UNC8153 是一种 NSD2(组蛋白-赖氨酸 N-甲基转移酶)的降解剂,其通过诱导NSD2的降解,具有350 nM的50%降解常数(DC50)值,并且在20 µM浓度下对NSD2具有选择性,而不选择NSD1和NSD3。在MM.1S多发性骨髓瘤细胞中,UNC8153 (10 µM) 能够诱导NSD2降解并减少组蛋白H3赖氨酸36位二甲基化(H3K36me2),这一效应可以被泛素激活酶抑制剂MLN4924所抑制。它减少了表达带有在1099位上谷氨酸到赖氨酸激活突变的NSD2(NSD2E1099K)的MM.1S细胞的增殖,但在20 µM浓度下,对表达野生型NSD2的MDA-MB-231、U2OS或HEK293细胞无效。UNC8153 (20 µM) 降低了在迁移实验中MM.1S细胞的附着能力。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1354 |
N-Acetyl-5-hydroxytryptamine
Normelatonin,N-乙酰-5-羟色胺,O-Demethylmelatonin,N-Acetylserotonin |
Trk receptor; Endogenous Metabolite | Metabolism; Tyrosine Kinase/Adaptors |
N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) 是褪黑激素的直接前体,能够有效激活TrkB 受体。 | |||
T8790 |
1-Methylhistamine dihydrochloride
|
Endogenous Metabolite | Metabolism |
1-Methylhistamine dihydrochloride 是组胺代谢物。 | |||
T4909 |
N-Acetyl-DL-methionine
N-乙酰-DL-蛋氨酸,N-乙酰-DL-甲硫氨酸 |
Others; Endogenous Metabolite | Metabolism; Others |
N-Acetyl-DL-methionine 是内源性代谢产物的一种。 | |||
T4120 |
N-Methylsarcosine
N,N-Dimethylglycine,N,N-Dimethylaminoacetic acid,Dimethylglycine,N,N-二甲基甘氨酸,DMG |
Endogenous Metabolite | Metabolism |
N-Methylsarcosine (Dimethylglycine) 被用作运动性能增强剂和免疫兴奋剂。它也被用于治疗自闭症、癫痫和线粒体疾病。它也被用作慢性阻塞性肺疾病(COPD)患者蛋白质降解的生物标志物。此外,它被用作鉴定、区分和表征氨基酸甲基转移酶的底物。它在甘氨酸基离子液体和乳化剂的发展中起着重要的作用。 |