目录号 | 产品详情 | 靶点 | |
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T2354 | Histone Methyltransferase | ||
UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平,IC50为 25 nM。 | |||
T17204 | Histone Methyltransferase | ||
UNC0321 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,在 ECSD 和 CLOT 测定中,Ki 为 63 pM,IC50 分别为 9 nM 和 6 nM。 UNC0321 抑制 GLP,在 ECSD 和 CLOT 试验中 IC50 分别为 15 nM 和 23 nM。 | |||
T7697 | Histone Methyltransferase Autophagy | ||
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。 | |||
TQ0232 | Histone Methyltransferase | ||
UNC0646 是一种有效的、选择性的同源蛋白赖氨酸甲基转移酶 G9a 和 GLP 抑制剂,IC50分别为 6 和 15 nM,对 G9a/GLP 的选择性比 SETD7、SUV39H2、SETD8 和 PRMT3 高。它降低 MDA-MB-231 细胞中H3K9me2的水平,IC50为 26 nM。 | |||
T7194 | Apoptosis DNA Methyltransferase Histone Methyltransferase | ||
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。 | |||
T1959 | Histone Methyltransferase Autophagy | ||
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。 | |||
T6820 | ATPase Others Reactive Oxygen Species Endogenous Metabolite mTOR | ||
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) 是神经代谢疾病 D-2-羟基戊二酸尿症中积累的主要代谢产物,可增加活性氧的产生。它是 α-酮戊二酸 (α-KG) 的弱竞争拮抗剂,可抑制多种α-KG 依赖性双加氧酶,Ki 为 10.87 mM。 | |||
T63351L | Histone Methyltransferase | ||
MS8511 HCl 是一种具有选择性和有效性的 G9a/GLP 共价抑制剂,通过靶向底物结合位点的半胱氨酸残基发挥作用。 MS8511 具有抗癌活性和抗增殖活性,可降低细胞内 H3K9me2 水平。MS8511 可用于研究包括脑癌、乳腺癌、卵巢癌在内的多种癌症。 | |||
T79776 | Histone Methyltransferase | ||
ZZM-1220是一种针对组蛋白赖氨酸甲基转移酶G9a/GLP的共价抑制剂,IC50值分别为458 nM和924 nM。该化合物能有效抑制H3K9me2在细胞中的作用,从而显著促进三阴性乳腺癌(TNBC)细胞的凋亡(apoptosis),同时在G2/M期阻断细胞周期的进程。 | |||
T22250 | Others | ||
5WKS 也称为ZINC97756584,是一种生物化学物质。它是G9a 蛋白抑制剂。G9A/EHMT2是一种核组蛋白赖氨酸甲基转移酶,催化H3K9me2,这是一种通常与转录基因沉默相关的可逆修饰。5WKS 可用于自身免疫性疾病或肿瘤的研究。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-03056 | LSD1 Protein, Human, Recombinant (His & GST) | Human | Baculovirus-Insect Cells | ||
LSD1 belongs to the flavin monoamine oxidase family. It contains 1 SWIRM domain and is a component of an RCOR/GFI/LSD1/HDAC complex. LSD1 interacts directly with GFI1 and GFI1B. LSD1 specifically removes histone H3K4me2 to H3K4me1 or H3K4me0 through a FAD-dependent oxidative reaction. When forming a complex with an androgen receptor (and possibly other nuclear hormone receptors), LSD1 changes its substrates to H3K9me2. Thus LSD1 is considered to act as a coactivator or a corepressor. It may play a role in the repression of neuronal genes. Alone, LSD1 is unable to demethylate H3 'Lys-4' on nucleosomes and requires the presence of RCOR1/CoREST to achieve such activity.
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TMPY-01869 | SIRT1 Protein, Human, Recombinant (His) | Human | E. coli | ||
SIRT1 belongs to the sirtuin family. Members of the sirtuin family are characterized by a sirtuin core domain and grouped into four classes. SIRT1 is included in class I of the sirtuin family. It is a NAD-dependent protein deacetylase, which regulates processes such as apoptosis and muscle differentiation by deacetylating key proteins. It deacetylates 'Lys-382' of p53/TP53 and impairs its ability to induce proapoptotic program and modulate cell senescence. SIRT1 also deacetylates TAF1B and thereby represses rDNA transcription by the RNA polymerase I. It is involved in HES1- and HEY2-mediated transcriptional repression. SIRT1 inhibits skeletal muscle differentiation by deacetylating PCAF and MYOD1. It may serve as a sensor of the cytosolic ratio of NAD(+)/NADH, which is essential in skeletal muscle cell differentiation. It also deacetylates 'Lys-16' of histone H4 (in vitro). Component of the eNoSC (energy-dependent nucleolar silencing) complex, a complex that mediates silencing of rDNA in response to intracellular energy status and acts by recruiting histone-modifying enzymes. The eNoSC complex is able to sense the energy status of cell: upon glucose starvation, elevation of NAD(+)/NADP(+) ratio activates SIRT1, leading to histone H3 deacetylation followed by dimethylation of H3 at 'Lys-9' (H3K9me2) by SUV39H1 and the formation of silent chromatin in the rDNA locus.
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