目录号 | 产品详情 | 靶点 | |
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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。 | |||
T16269 | DNA Methyltransferase Dehydrogenase Parasite | ||
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 | Apoptosis DNA Methyltransferase | ||
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 | 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 | Histone Methyltransferase | ||
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(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 | DNA Methyltransferase Histone Methyltransferase | ||
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 | DNA Methyltransferase | ||
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. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-03046 | APCDD1 Protein, Human, Recombinant (hFc) | Human | HEK293 | ||
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. Moreover, DNMT3a, but not DNMT1 or DNMT3b, was the major DNA methyltransferase that facilitated hyper-methylation of DNA in the APCDD1 promoter, thus reducing APCDD1 mRNA levels in OS tissues. Importantly, ectopic expression of APCDD1 suppressed activity of the Wnt/beta-Catenin signaling pathway in OS cells and inhibited their invasion and reversed their EMT-like properties, while depletion of APCDD1 promoted invasion and metastasis of osteosarcoma cells in vitro and in vivo. That APCDD1 modulates the gene expression of Wnt- and EK-related signaling molecules at the cap stage of tooth development, and is involved in tooth cusp patterning by modulating the epithelial rearrangement in the IEE. In hair follicle cells APCDD1 inhibits the canonical WNT/beta-Catenin pathway and its inactivation is associated with an autosomal dominant form of hair loss. APCDD1 sustains the expression and activation of beta-Catenin.
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TMPJ-01115 | GALNT3 Protein, Human, Recombinant (His) | Human | Human Cells | ||
Polypeptide N-acetylgalactosaminyltransferase 3(GALNT3) belongs to the glycosyltransferase 2 family and galNAc-T subfamily. It expressed in organs that contain secretory epithelial glands and it highly expressed in pancreas, skin, kidney and testis. There are two conserved domains in the glycosyltransferase region: the N-terminal domain (domain A, also called GT1 motif), which is probably involved in manganese coordination and substrate binding and the C-terminal domain (domain B, also called Gal/GalNAc-T motif), which is probably involved in catalytic reaction and UDP-Gal binding .This protein plays a major role in regulating phosphate levels within the body (phosphate homeostasis). Among its many functions, phosphate plays a critical role in the formation and growth of bones in childhood and helps maintain bone strength in adults.
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TMPK-00989 | APCDD1 Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
Adenomatosis polyposis coli downregulated 1 (APCDD1), a negative regulator of Wnt signaling, was examined to understand detailed mechanisms underlying Wnt signaling tooth development. In situ hybridization showed that Apcdd1 was expressed in the condensed mesenchyme at the bud stage, and in the inner enamel epithelium (IEE), including enamel knot (EK) at the cap stage. APCDD1 modulates the gene expression of Wnt- and EK-related signaling molecules at the cap stage of tooth development, and is involved in tooth cusp patterning by modulating the epithelial rearrangement in the IEE.
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TMPK-00311 | APCDD1 Protein, Human, Recombinant (His) | Human | HEK293 | ||
Adenomatosis polyposis coli downregulated 1 (APCDD1), a negative regulator of Wnt signaling, was examined to understand detailed mechanisms underlying Wnt signaling tooth development. In situ hybridization showed that Apcdd1 was expressed in the condensed mesenchyme at the bud stage, and in the inner enamel epithelium (IEE), including enamel knot (EK) at the cap stage. APCDD1 modulates the gene expression of Wnt- and EK-related signaling molecules at the cap stage of tooth development, and is involved in tooth cusp patterning by modulating the epithelial rearrangement in the IEE.
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