35
7
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1904 |
SGI-1027
DNA Methyltransferase Inhibitor II,SGI1027 |
Apoptosis; DNA Methyltransferase | Apoptosis; Chromatin/Epigenetic |
SGI-1027 (DNA Methyltransferase Inhibitor II) 是一种 DNA 甲基转移酶(DNMT)抑制剂,对以 poly(dI-dC) 为底物的 DNMT3B,DNMT3A 和 DNMT1 的IC50值分别为 7.5 μM,8 μM 和 12.5 μM。 | |||
T15080 |
DC-05
|
DNA Methyltransferase; Histone Methyltransferase | Chromatin/Epigenetic |
DC-05 是一种DNMT1的抑制剂,IC50和Kd 值分别为 10.3 和 1.09 μM。 | |||
T7194 |
CM-272
|
Apoptosis; DNA Methyltransferase; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
CM-272 是一种可逆底物竞争性双重G9a/DNA 甲基转移酶选择性抑制剂,具有抗肿瘤活性。它抑制细胞增殖并促进细胞凋亡,诱导干扰素刺激的基因和免疫原性细胞死亡。它抑制G9a、DNMT1、DNMT3A、DNMT3B 和GLP,IC50分别为 8 nM、382 nM、85 nM、1200 nM 和 2 nM。 | |||
T11469 |
GSK-3484862
|
DNA Methyltransferase | Chromatin/Epigenetic |
GSK-3484862 是 有效的 DNA 甲基转移酶 Dnmt1的非共价抑制剂。GSK-3484862 通过诱导 DNA 低甲基化起抗癌作用。GSK-3484862 介导小鼠胚胎干细胞的整体去甲基化。 | |||
T5198 |
Bobcat339
盐酸Bobcat339,Bobcat339 hydrochloride |
DNA Methyltransferase | Chromatin/Epigenetic |
Bobcat339 是一种基于胞嘧啶的选择性TET 酶抑制剂,抑制TET1和TET2的IC50值分别为 33 和 73 μM。它可作为靶向 DNA 甲基化和基因转录新疗法的起点,用于表观遗传学领域研究。 | |||
T2495 |
Lomeguatrib
罗米鲁曲,PaTrin-2 |
DNA Methyltransferase; DNA Alkylation | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Lomeguatrib (PaTrin-2) 是修饰鸟嘌呤碱基,是MGMT 有效抑制剂,可抑制 DNA 修复蛋白 O(6)-烷基鸟嘌呤-DNA 烷基转移酶 (MGMT) 的活性。在非细胞体系和 MCF-7 细胞体系中,IC50值分别为 9 nM 和约 6 nM。 | |||
T8967 |
SW155246
|
DNA Methyltransferase | Chromatin/Epigenetic |
SW155246 是选择性 DNA 甲基转移酶 (DNMT1) 抑制剂,能够抑制 hDNMT1 (IC50:1.2 μM) 以及 mDNMT3A (IC50:38 μM)。它能够促使 A549细胞中肿瘤抑制基因 RASSF1的重新表达,可用于研究癌症和其他疾病。 | |||
T7718 |
5-Fluoro-2'-deoxycytidine
5-氟脱氧胞苷,FdCyd,2'-DEOXY-5-FLUOROCYTIDINE |
DNA Methyltransferase | Chromatin/Epigenetic |
5-Fluoro-2'-deoxycytidine (2'-DEOXY-5-FLUOROCYTIDINE) 是一种 DNA 甲基转移酶(DNMT) 抑制剂,是氟嘧啶核苷类似物。它是胸苷酸合酶抑制剂 5-fluoro-2′-dUMP 的肿瘤选择性前药。 | |||
T2169 |
Zebularine
NSC309132,4-Deoxyuridine |
DNA Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
Zebularine (4-Deoxyuridine) 是一种 DNA 甲基化抑制剂,还抑制胞苷脱氨酶。它通过以共价水合物的形式与活性大小结合,充当胞苷脱氨酶的过渡态类似物抑制剂。 | |||
T9573 |
GSK3685032
|
DNA Methyltransferase | Chromatin/Epigenetic |
GSK-3685032 是一种非时间依赖、非共价、选择性的、可逆的DNMT1抑制剂,IC50=0.036 μM。它诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。 | |||
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。 | |||
T7840 |
2',3',5'-triacetyl-5-Azacytidine
Nsc291930,三乙酰基-阿扎胞苷 |
DNA Methyltransferase; Others | Chromatin/Epigenetic; Others |
2',3',5'-triacetyl-5-Azacytidine (Nsc291930) 是 5-Azacytidine 的前药,口服有活性。 5-Azacytidine 是 DNA 甲基转移酶的抑制剂。 | |||
T0192 |
Levetiracetam
左乙拉西坦,UCB L059,SIB-S1 |
DNA Methyltransferase; Others; Calcium Channel | Chromatin/Epigenetic; Membrane transporter/Ion channel; Metabolism; Others |
Levetiracetam (SIB-S1) 是一种化学增敏剂,增强 Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。它调节 HDAC 水平,最终使 MGMT 沉默从而提高 Temozolomide 的有效性。它是一种抗癫痫药,可结合突触小泡蛋白 SV2A。 | |||
T3089 |
6-Thioguanine
6-TG,2-Amino-6-purinethiol,2-Amino-6-mercaptopurine,Thioguanine,6-硫代鸟嘌呤 |
Apoptosis; DNA Methyltransferase; SARS-CoV; Endogenous Metabolite; DUB; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; Ubiquitination |
6-Thioguanine (2-Amino-6-purinethiol) 是一种抗白血病和免疫抑制剂,是 SARS 和 MERS 冠状病毒木瓜样蛋白酶抑制剂,也抑制 USP2的活性,IC50值分别为 25 μM 和 40 μM。 | |||
T16269 |
Nanaomycin A
|
DNA Methyltransferase; Dehydrogenase; Parasite | Chromatin/Epigenetic; Metabolism; Microbiology/Virology |
Nanaomycin A 是一种醌类抗生素,可重新激活人类癌细胞中沉默的肿瘤抑制基因。 Nanaomycin A 是 DNMT3B 的特异性抑制剂 (IC50 = 500 nM)。 | |||
T28663 |
Sarmustine
NSC-364432,SarCNU,Sarcosinamide,NSC 364432,NSC364432 |
||
Sarmustine (SarCNU) 是一种具有抗癌活性的烷化剂,通过 p53 依赖性和 p53 非依赖性途径抑制前列腺癌细胞的生长。Sarmustine 在体外介导 P140K 甲基鸟嘌呤-DNA-甲基转移酶转导的人 CD34(+)细胞的选择。 | |||
TNU0425 |
2’-Deoxy-2’-fluoro-β-D-arabinocytidine hydrochloride
|
DNA Methyltransferase | Chromatin/Epigenetic |
2’-Deoxy-2’-fluoro-β-D-arabinocytidine hydrochloride 是一种胞嘧啶核苷类似物,对DNA 甲基转移酶具有抑制作用 ,具有潜在的抗代谢和抗肿瘤活性。 | |||
T60322 |
Procainamide
Biocoryl,Novocainamide |
DNA Methyltransferase | Chromatin/Epigenetic |
Procainamide (Novocainamide) 是 DNA 甲基转移酶 1 (DNMT1) 的特异性强效抑制剂。Procainamide 是一种 1A 类抗心律失常药物。Procainamide 具有研究癌症和心律失常的潜力。 | |||
T1613 |
Hydralazine hydrochloride
Hydralazine HCl,Apresoline,盐酸肼屈嗪 |
MAO; HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism; Neuroscience |
Hydralazine hydrochloride (Apresoline) 是一种直接作用的血管舒张剂,可抗高血压。 | |||
T25594 | Laccaic acid A | ||
Laccaic acid A is a direct, DNA-competitive DNA methyltransferase 1 inhibitor. | |||
T10840L |
CM-579
|
DNA Methyltransferase; Histone Methyltransferase | Chromatin/Epigenetic |
CM-579 是首创的、可逆的,G9a 和 DNA 甲基转移酶 (DNMT) 的双抑制剂,其 IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。 | |||
T23968 |
DC_501
DC 501,DC501 |
||
DC_501 is a selective non-nucleoside DNA methyltransferase 1 inhibitor. | |||
T15081 | DC_517 | DNA Methyltransferase | Chromatin/Epigenetic |
DC_517 is an inhibitor of DNA methyltransferase 1 (DNMT1) ( IC50: 1.7 μM; Kd: 0.91 μM). | |||
T26496 |
AA-CW236
AA-CW 236,AACW-236,AACW236,AACW 236,AA-CW-236 |
||
AA-CW236 is a covalent inhibitor of human O(6)-alkylguanine DNA methyltransferase (MGMT). | |||
T60476 |
2′-Deoxy-5-nitrocytidine
|
||
2′-Deoxy-5-nitrocytidine 是一种 DNA 甲基转移酶(DNMT)的抑制剂,可用于癌症领域研究。 | |||
T62643 |
DY-46-2
|
||
DY-46-2 是一种强选择性、高效的新型非核苷 DNA 甲基转移酶 3A (DNMT3A) 抑制剂 (IC50: 1.3 μM)。 | |||
T40560 | Benzyl selenocyanate | ||
Benzyl selenocyanate is a chemopreventive agent that effectively inhibits chemically induced tumors at both initiation and postinitiation stages in animal models. It acts as a potent inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an IC50 of 8.4 μM. | |||
T82614 | DAM-IN-1 | DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
DMA-IN-1是一种DNA腺嘌呤甲基转移酶抑制剂,具有48 μM的IC50值。同时,它能够抑制Caulobacter的生长,其MIC为35 μM。 | |||
T27395 |
Furamidine dihydrochloride
DB 75, DB75, NSC 305831, WR199385,Furamidine HCl |
||
Furamidine is a cell-permeable, selective inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine targets the enzyme active site and is primarily competitive with t | |||
T11338 |
Furamidine
DB75,NSC 305831 |
Others | Others |
Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and ... | |||
T36100 | K-TMZ | ||
K-TMZ is a DNA alkylating agent. It increases the concentration of O6-methylated deoxyguanosine in U87 glioblastoma multiforme (GBM) cells in a concentration-dependent manner. K-TMZ reduces cell viability of GBM cell lines lacking (IC50s = 18-44 μM) or expressing O6-methylguanine DNA methyltransferase (MGMT; IC50s = 115-240 μM). K-TMZ can cross the blood-brain barrier and increases survival in a Br23c mouse xenograft model of GBM when administered at a dose of 14.9 mg/kg. | |||
T73274 |
CamA-IN-1
|
||
CaMA-IN-1 是一种Clostridioides difficile 特异性 DNA 腺嘌呤甲基转移酶(CamA)抑制剂。CamA-IN-1 对 CamA 具有抑制作用,IC50和Kd 值分别为 0.4 μM 和 0.2 μM 。CaMA-IN-1 可用于Clostridioides difficile 感染(CDI)的研究。 | |||
T35413 |
(6R,S)-5,6,7,8-Tetrahydrofolic Acid (hydrochloride)
|
||
(6R,S)-5,6,7,8-Tetrahydrofolic acid (THFA), the reduced form of folic acid, serves as a cofactor in methyltransferase reactions and is the major one-carbon carrier in one carbon metabolism. Its metabolites participate in the synthesis of thymidine for incorporation into DNA or the synthesis of purines, as well as in the formation of methionine, which can be converted to the ubiquitous methyl donor, S-adenosylmethionine . THFA has also been used to study the activation of metabolite-binding ribos... | |||
T79035 |
PRMT5-IN-28
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-28(化合物36)是一种PRMT5抑制剂,能够调控包含基因转录、mRNA剪接、DNA修复、蛋白质定位、细胞命运和信号传导等过程的蛋白质精氨酸甲基化。PRMT5的异常活性与癌症细胞的增殖、抗凋亡、侵袭转移能力增强及免疫逃逸机制的影响相关。 | |||
T10840 |
CM-579 trihydrochloride (1846570-40-8 free base)
CM-579 trihydrochloride |
DNA Methyltransferase | Chromatin/Epigenetic |
CM-579 trihydrochloride is a first-in-class reversible and dual inhibitor of G9a and DNMT (IC50s: 16 nM, 32 nM) with potent in vitro cellular activity in a wide range of cancer cells. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3606 |
γ-Oryzanol
谷维素,Gamma-Oryzanol,Oliver,γ-谷维素,Gammariza |
DNA Methyltransferase | Chromatin/Epigenetic |
γ-Oryzanol (Gamma-Oryzanol) 是一种从米糠油中分离出来的营养提取物,是含有甾醇和阿魏酸的混合物,有助于破坏皮肤中的自由基。它有效抑制小鼠纹状体中的 DNA 甲基转移酶(DNMTs)。 它抑制DNMT1和DNMT3a,IC50分别为 3.2 和 22.3 μM。 | |||
T3717 |
Hinokitiol
4-Isopropyltropolone,桧木醇,β-thujaplicin,β-桧木醇 |
DNA Methyltransferase; Virus Protease; Estrogen/progestogen Receptor; Nrf2 | Chromatin/Epigenetic; Endocrinology/Hormones; Immunology/Inflammation; Microbiology/Virology |
Hinokitiol (4-Isopropyltropolone) 是从日本扁柏中分离到的一种挥发油成分,可抑制紫外线 B 诱导的角质形成细胞凋亡,可调节雌激素受体信号传导并抑制人乳腺癌细胞的增殖。它具有抗感染、抗氧化及抗肿瘤等活性。 | |||
T7457 |
5-Methyl-2'-deoxycytidine
5-Methyldeoxycytidine,5-甲基-2'-脱氧胞苷,5MedCyd |
DNA Methyltransferase; Endogenous Metabolite | Chromatin/Epigenetic; Metabolism |
5-Methyl-2'-deoxycytidine (5MedCyd) 是嘧啶核苷,当掺入到单链 DNA 中时,可以顺式作用以从头发出信号。 | |||
T1508 |
Decitabine
Dacogen,NSC 127716,地西他滨,Deoxycytidine,5-Aza-2'-deoxycytidine |
Apoptosis; Nucleoside Antimetabolite/Analog; DNA Methyltransferase | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Decitabine (Deoxycytidine) 是脱氧胞苷类似物,一种 DNA 甲基转移酶抑制剂,具有口服活性。Decitabine 具有抗肿瘤活性和抗代谢活性。Decitabine 诱导细胞周期阻滞和凋亡。 | |||
T1339 |
5-Azacytidine
阿托胞苷,Azacitidine,NSC 102816,Mylosar,Ladakamycin,5-氮杂胞苷,5-AzaC |
Nucleoside Antimetabolite/Analog; DNA Methyltransferase; Antibacterial; Antibiotic; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology |
5-Azacytidine (Ladakamycin) 是一种胞苷核苷类似物,一种 DNA 甲基化抑制剂,具有特异性。5-Azacytidine 通过降低 DNA 甲基化水平调节基因表达。5-Azacytidine 可以诱导细胞自噬,具有抗肿瘤活性。 | |||
T2988 |
(-)-Epigallocatechin Gallate
Epigallocatechol Gallate,(-)-表没食子儿茶素没食子酸酯,EGCG |
Ferroptosis; Reactive Oxygen Species; HIV Protease; Mitochondrial Metabolism; Endogenous Metabolite; Autophagy | Apoptosis; Autophagy; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome |
(-)-Epigallocatechin Gallate (EGCG) 是茶类黄酮,具有强大的抗氧化,抗炎和抗癌作用。它可抑制EGFR 信号传导,有抗癌作用。它是谷氨酸脱氢酶 1/2 抑制剂。它通过激活细胞色素c 氧化酶来诱导氧化磷酸化。 | |||
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。 |