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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
T16813 |
RX-3117
fluorocyclopentenylcytosine,TV-1360 |
Nucleoside Antimetabolite/Analog | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
RX-3117 (fluorocyclopentenylcytosine) 是一种新型的胞苷类似物,在几种癌细胞系中显示出抗癌活性,包括对吉西他滨耐药的变体。 | |||
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。 | |||
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。 | |||
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。 | |||
T12261 |
NSC232003
|
E1/E2/E3 Enzyme | Ubiquitination |
NSC232003 是高效的UHRF1抑制剂,能够抑制 DNA 甲基化,并破坏 DNMT1/UHRF1 相互作用。 | |||
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). | |||
T11682 |
Isofistularin-3
|
Others; ADC Cytotoxin | Antibody-drug Conjugate/ADC Related; Others |
Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. | |||
T74887 |
GSK3735967
|
Others | Others |
GSK3735967为选择性、可逆的非核苷类DNMT1抑制剂,具备平面二氰基吡啶核心,专一性嵌入DNMT1所结合的半甲基化CpG双核苷酸中。该化合物包含三个结合位点,其中之一可与组蛋白H4K20me3相结合。 | |||
T81432 |
PNMT-IN-1
|
Others | Others |
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。 | |||
T11185 |
EML741
|
Histone Methyltransferase | Chromatin/Epigenetic |
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. | |||
T39648 |
(R)-GSK-3685032
|
Others | Others |
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a first-in-class, non-time-dependent, non-covalent, reversible, selective DNMT1 inhibitor with an IC 50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation and inhibition of cancer cell growth. | |||
T73257 |
USP7-IN-9
|
Others | Others |
USP7-IN-9是一种高效USP7抑制剂,其IC50值为40.8 nM。该化合物可诱导RS4; 11 细胞发生(apoptosis),并使细胞周期在G0/G1及S期停滞。此外,USP7-IN-9能够降低癌症相关蛋白MDM2和DNMT1的表达量,同时增加抑癌蛋白p53与p21的表达量。 | |||
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。 | |||
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 |
---|---|---|---|
T2210 |
Genipin
京尼平,(+)-Genipin |
Others; Autophagy | Autophagy; Others |
Genipin ((+)-Genipin) 是衍生自黄栀果实的天然交联剂,可抑制细胞中的 UCP2 (解偶联蛋白 2)。它有蛋白质调节、抗肿瘤、抗炎症、免疫抑制、抗血栓形成和对海马神经元保护的多种生物活性,可研究 2 型糖尿病。 | |||
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。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-03046 |
APCDD1 Protein, Human, Recombinant (hFc)
HYPT1,B7323,adenomatosis polyposis coli down-regula... |
Human | HEK293 Cells |
Osteosarcoma (OS) is the most common type of bone tumor in children and adults. The expression of APCDD1, a Wnt antagonist, was reduced in OS tissues and cells compared to adjacent normal tissue and osteoblast cells, respectively. Mechanistically, this was due to increased levels of methylation in the promoter region of the APCDD1 gene. Consistently, the DNA methyltransferase inhibitor 5-AZA-dC, reduced DNA methylation in the APCDD1 promoter, and restored APCDD1 expression in OS tissue and cells... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMID-0192 |
Procainamide-d10
|
||
Procainamide-d10 是 Procainamide 的氘代化合物。Procainamide 的 CAS 号为 51-06-9。Procainamide 是一种特异性强效的 DNA 甲基转移酶 1 (DNMT1) 抑制剂。普鲁卡因胺是一种 1A 类抗心律失常药物。Procainamide 具有研究癌症和心律失常的潜力。 |