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35

抑制剂 & 化合物

4

天然产物

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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。

化合物

Metoprine
Cat.No: T8548
Synonym:
Target: Histone Methyltransferase, Antifolate, Histamine Receptor
Amodiaquine
Cat.No: T8381
Synonym:
Target: Others, Histone Methyltransferase, Parasite
RG108
Cat.No: T2038
Synonym: N-Phthalyl-L-tryptophan
Target: DNA Methyltransferase
XY1
Cat.No: T7157
Synonym: N-2-萘基-N'-[2-氧代-2-(1-吡咯烷基)乙基]脲
Target: Histone Methyltransferase
AMI-1
Cat.No: T2352
Synonym:
Target: Histone Methyltransferase
Amodiaquine dihydrochloride dihydrate
Cat.No: T0381
Synonym: Amodiaquine hydrochloride,阿莫地喹盐酸盐,Amodiaquin dihydrochloride dihydrate
Target: Histone Methyltransferase, Parasite, Histamine Receptor
LY 78335
Cat.No: T22956
Synonym: 1-(2,3-Dichlorophenyl)ethanamine hydrochloride
Target: Others
Arazine
Cat.No: T10363
Synonym: N-Acetyl-S-farnesyl-L-cysteine
Target: Others
BIX-01294
Cat.No: T7697
Synonym:
Target: Histone Methyltransferase, Autophagy
JBSNF-000088
Cat.No: T8106
Synonym: JBSNF000088
Target: Others
NNMTi
Cat.No: T8760
Synonym: 5-Amino-1-methylquinolinium
Target: Others
BIX-01294 trihydrochloride
Cat.No: T1959
Synonym: BIX 01294
Target: Histone Methyltransferase, Autophagy
JBSNF-000028
Cat.No: T72947
Synonym: JBSNF-000028 free base
Target: Others
Lifibrate
Cat.No: T27831
Synonym:
Target:
PDAT
Cat.No: T24604
Synonym: Propyl Dimethyl Amino Tryptamine
Target:
LY 87130
Cat.No: T27924
Synonym: LY87130,LY-87130
Target:
MS2734
Cat.No: T71922
Synonym:
Target:
LY 134046
Cat.No: T27872
Synonym: LY-134046,LY134046,Lilly 134046
Target:
SKF 91488 dihydrochloride
Cat.No: T23367
Synonym:
Target: Others
Quinacrine acetate
Cat.No: T68694
Synonym:
Target:
N-acetyl-S-geranylgeranyl-L-Cysteine
Cat.No: T37693
Synonym:
Target:
Chlorpromazine Sulfone Hydrochloride
Cat.No: T70105
Synonym:
Target:
Bisubstrate Inhibitor 78
Cat.No: T36802
Synonym:
Target:
BAY-598 R-isomer
Cat.No: T26744
Synonym: BAY598 R-isomer,BAY 598 R-isomer
Target:
DC 432
Cat.No: T83949
Synonym:
Target:
JBSNF-000028 TFA
Cat.No: T78163
Synonym:
Target: Others
JBSNF-000028 hydrochloride
Cat.No: T78164
Synonym:
Target: Others
MS2177
Cat.No: T28114
Synonym: MS 2177,MS-2177
Target:
Amodiaquine hydrochloride
Cat.No: T22242
Synonym:
Target:
JBSNF-000028 free base
Cat.No: T82011
Synonym:
Target:
NNMT-IN-3
Cat.No: T64189
Synonym:
Target:
DC432 TFA
Cat.No: T83713
Synonym:
Target:
NNMT-IN-4
Cat.No: T81661
Synonym:
Target:
PNMT-IN-1
Cat.No: T81432
Synonym:
Target:
UNC8153 TFA
Cat.No: T83867
Synonym:
Target:
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。

天然产物

N-Acetyl-5-hydroxytryptamine
Cat.No: T1354
Synonym: Normelatonin,N-乙酰-5-羟色胺,O-Demethylmelatonin,N-Acetylserotonin
Target: Trk receptor, Endogenous Metabolite
1-Methylhistamine dihydrochloride
Cat.No: T8790
Synonym:
Target: Endogenous Metabolite
N-Acetyl-DL-methionine
Cat.No: T4909
Synonym: N-乙酰-DL-蛋氨酸,N-乙酰-DL-甲硫氨酸
Target: Others, Endogenous Metabolite
N-Methylsarcosine
Cat.No: T4120
Synonym: N,N-Dimethylglycine,N,N-Dimethylaminoacetic acid,Dimethylglycine,N,N-二甲基甘氨酸,DMG
Target: Endogenous Metabolite
TargetMol Loading
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