Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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)。 | |||
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。 | |||
T15169 |
DS-437
|
Others | Others |
DS-437 is a dual PRMT5/7 inhibitor (IC50s: 6 μM). DS-437 also inhibits DNMT3A and DNMT3B (IC50s: 52 and 62 μM). DS-437 inhibits the methylation of FOXP3. | |||
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. | |||
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。 | |||
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. |