Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2352 |
AMI-1
|
Histone Methyltransferase | Chromatin/Epigenetic |
AMI1 是一种有效的、可逆的、细胞渗透性的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂,对人 PRMT1 和酵母 Hmt1p 作用的 IC50值分别为 8.8 和 3.0 μM。它通过阻断肽-底物结合对 PRMTs 发挥抑制作用。 | |||
T61338 |
MS023 dihydrochloride
MS023 2HCl |
Histone Methyltransferase | Chromatin/Epigenetic |
MS023 dihydrochloride (MS023 2HCl) 是一种具有选择性、细胞活性和高效性的人I 型蛋白精氨酸甲基转移酶 (PRMTs)抑制剂,具有抗肿瘤活性,抑制 PRMT1,PRMT3,PRMT4,PRMT6和PRMT8,增加离体培养的 MuSC 的增殖能力,可用于研究乳腺癌。 | |||
T11500L |
GSK3368715 dihydrochloride
EPZ019997 dihydrochloride,GSK3368715 2HCl,EPZ019997 2HCl |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 是一种具有口服活性和高效性的 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂 ,具有抗癌和抗肿瘤活性,抑制PRMT1,PRMT3,PRMT4,PRMT6,PRMT8的活性,可用于研究晚期实体肿瘤。 | |||
T4013 |
SGC2085 HCl
|
Histone Methyltransferase | Chromatin/Epigenetic |
SGC2085 HCl 是一种有效的选择性辅激活剂相关的精氨酸甲基转移酶 1 (CARM1) 抑制剂,IC50 为 50 nM,选择性比其他 PRMT 高出数倍。 CARM1 是结直肠癌中 Wnt/β-catenin 转录和肿瘤转化的重要正调节因子,也是雌激素刺激的乳腺癌生长的关键因素,其耗竭导致体内髓性白血病细胞增殖减少。 | |||
T70094 |
MS-049 oxalate salt
|
||
MS-049 oxalate salt is a potent and selective inhibitor of protein arginine methyltransferases (PRMTs) PRMT 4 and PRMT6. | |||
T22239 | AMI-1, free acid | ||
AMI-1 free acid 是一种有效的,具有细胞渗透性和可逆的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂,对人 PRMT1 和酵母 Hmt1p 作用的 IC50值分别为 8.8 μM 和 3.0 μM。AMI-1 free acid 通过阻断肽-底物结合发挥 PRMTs 抑制作用。 | |||
T69580 |
SGC6870
|
||
SGC6870 is a novel potent, selective, and cell-active inhibitor of PRMT6 with IC50 of 77 ± 6 nM, being selective over all other PRMTs and 23 methyltransferases. | |||
T11500 |
GSK3368715
EPZ019997 |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity. | |||
T36981 |
GSK 591 dihydrochloride
|
||
Potent and selective PRMT5 inhibitor (IC50 = 4 nM). Selective for PRMT5 over a panel of other PRMTs and lysine methyltransferases. Inhibits proliferation of mantle cell lymphoma (MCL) in vitro. To request the negative control for GSK 591, please fill out the SGC 2096 request form on the SGC website. | |||
T36976 | SGC 6870 | ||
Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM). Exhibits selectivity over all other PRMTs and 23 methyltransferases. In HEK293T cells overexpressing PRMT6, inhibits asymmetric dimethylation of H3R2 (IC50 = 0.8 μM) Negative control SGC 6870N (Cat. No. 7184) also available. | |||
T4393 |
MS049 2HCl (1502816-23-0(free base))
|
Histone Methyltransferase | Chromatin/Epigenetic |
MS049 2HCl (1502816-23-0(free base)) 是一种有效的选择性 PRMT4 (IC50 = 34 nM) 和 PRMT6 (IC50 = 43 nM) 抑制剂。它对其他 I 型 PRMT 的活性较低(对于 PRMT1、PRMT3 和 PRMT8,IC50分别>130、>220 和 1.6 μM,),并且对 II 型或 III 型 PRMT 没有抑制作用,也没有对任何其他甲基转移酶或非表观遗传靶标进行测试。 | |||
T61862 | PRMT5-IN-19 | ||
PRMT5-IN-19 (Compound 41) is a potent orally active PRMT5 inhibitor, exhibiting selectivity towards the SAM-binding pocket of PRMT5 with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). It effectively blocks methyltransferase activity and demonstrates high specificity against other PRMTs and PKMTs. PRMT5-IN-19 exerts anti-proliferative effects through the induction of apoptosis and holds potential in cancer-related research [1]. | |||
T70990 |
ADMA-d6
|
||
NG,NG-dimethyl-L-arginine-d6 (ADMA-d6) (hydrochloride) is intended for use as an internal standard for the quantification of NG,NG-dimethyl-L-arginine by GC- or LC-MS. ADMA is an endogenous inhibitor of nitric oxide synthase (NOS). It is formed from arginine by protein arginine methyltransferases (PRMTs) and degraded by dimethylarginine dimethylaminohydrolases (DDAHs) and alanine-glyoxylate aminotransferase 2 (AGXT2). ADMA levels are increased concomitant with an increase in blood pressure in Da... |