Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T38421 |
PRMT1-IN-1
PRMT1-IN-1 |
||
PRMT1-IN-1 is a PRMT1 inhibitor. | |||
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。 | |||
T27133 |
DCLX069
DCLX 069,DCLX-069 |
Histone Methyltransferase | Chromatin/Epigenetic |
DCLX069 是一种选择性蛋白精氨酸甲基转移酶 1 抑制剂,IC50值为 17.9 µM,对 PRMT4 和 PRMT6 的活性较低。它可有效阻断乳腺癌、肝癌和急性髓性白血病细胞系中的细胞增殖。 | |||
T7697 |
BIX-01294
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
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。 | |||
T1959 |
BIX-01294 trihydrochloride
BIX 01294 |
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
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。 | |||
T21826 |
TC-E 5003
NSC 30176 |
Histone Methyltransferase | Chromatin/Epigenetic |
TC-E 5003 (NSC-30176) 是选择性 PRMT1抑制剂,其 IC50值为1.5 µM。它在 TLR4 信号传导中具有抗炎特性。 | |||
T2097 |
C-7280948
C7280948 |
Histone Methyltransferase | Chromatin/Epigenetic |
C-7280948 是一种选择性有效的PRMT1抑制剂,IC50值 12.75 μM。 | |||
T6900 |
MS023
|
Histone Methyltransferase | Chromatin/Epigenetic |
MS023 是一种有效的、选择性的、细胞活性的 I 型 PRMT 抑制剂,对 PRMT1、PRMT3、PRMT4、PRMT6和 PRMT8的 IC50分别为 30、119、83、4 和 5 nM。 | |||
T10682L |
CARM1-IN-1
CARM1-IN-7G |
Histone Methyltransferase | Chromatin/Epigenetic |
CARM1-IN-1 (CARM1-IN-7G) 是 CARM1 的选择性抑制剂,IC50 为 8.6 μM。 CARM1-IN-1 对 PRMT1 和 SET7 的活性较弱,IC50 > 600 μM。 | |||
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。 | |||
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。 | |||
T22342 |
GSK3368715 3HCl
EPZ019997 3HCl,GSK3368715(EPZ019997) |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM. | |||
T22325 |
EPZ020411 hydrochloride
EPZ020411 HCl |
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ020411 hydrochloride 是一种选择性的和有效的 PRMT6抑制剂,IC50=10 nM。 | |||
T77787 |
MS023 trihydrochloride
MS023 3HCl |
Histone Methyltransferase | Chromatin/Epigenetic |
MS023 trihydrochloride (MS023 3HCl) 是一种具有选择性和有效性的人I型蛋白精氨酸甲基转移酶 (PRMT)抑制剂,具潜在的抗癌活性,对 PRMT1、PRMT3、PRMT4、PRMT6 和 PRMT8 具有抑制作用,可用于研究癌症。 | |||
T81399 | PRMT4-IN-2 | ||
PRMT4-IN-2(化合物55)是一种针对蛋白质精氨酸甲基转移酶(PRMT)系列的抑制剂,其半抑制浓度(IC50s)分别对应PRMT4为92 nM,PRMT6为436 nM,PRMT1为460 nM,PRMT8为823 nM,PRMT3为1.386 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。 | |||
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. | |||
TP2041 |
C 21
|
||
Selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.8 μM). Exhibits five-fold selectivity for PRMT1 over PRMT6 and >250-fold selectivity over PRMT3 and CARM1. | |||
T27395 |
Furamidine dihydrochloride
DB 75, DB75, NSC 305831, WR199385,Furamidine HCl |
||
Furamidine is a cell-permeable, selective inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine targets the enzyme active site and is primarily competitive with t | |||
T11338 |
Furamidine
DB75,NSC 305831 |
Others | Others |
Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and ... | |||
T64186 |
CARM1-IN-1 hydrochloride
|
||
CARM1-IN-1 hydrochloride 是一种高效的、选择性的 CARM1 抑制剂 (IC50: 8.6 μM),对 PRMT1 和 SET7 抑制作用很低。 | |||
T10967 |
DC_C66
|
Others | Others |
DC_C66 DC_C66 has good selectivity for CARM1, PRMT1 (IC50 = 21μM), PRMT6 (IC50 = 47μM) and PRMT5. It is a cell-permeable, selective co-activator related arginine methyltransferase 1 (CARM1) inhibitor with IC50 of 1.8 μM. | |||
T19243 |
CMP-5 hydrochloride
|
Others | Others |
CMP-5 hydrochloride is a potent and selective PRMT5 inhibitor, while displays no activity against PRMT1/4/7 enzymes. It selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. | |||
T23030 |
MS023 (hydrochloride) (1831110-54-3 free base)
MS023 (hydrochloride) |
Others | Others |
MS023 is a type I PRMT inhibitor (IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectively). | |||
T72013 |
Epigenetic Multiple Ligand
|
||
Epigenetic Multiple Ligand is a cell-permeable inhibitor of substrate processing by several chromatin-associated enzymes, including SIRT1/2, H3/SET7, H3/p300/CBP, H4/RmtA, PABP1/CARM1, and H4/PRMT1. It acts by inducing either apoptosis or granulocytic differentiation. | |||
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。 | |||
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。 | |||
T36802 |
Bisubstrate Inhibitor 78
|
||
Bisubstrate inhibitor 78 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50= 1.41 μM).1It binds the NNMT active site in the binding pockets for the NNMT substrates S-adenosyl-L-methionine (SAM) and nicotinamide . Bisubstrate inhibitor 78 is selective for NNMT over histone-lysine N-methytransferase NSD2 and protein arginine methyltransferase 1 (PRMT1; IC50s = >50 μM for both). It reduces levels of 1-methylnicotinamide in, and inhibits proliferation of, HSC-2 oral cancer cells when us... | |||
T4314 |
EPZ020411
EPZ020411 2HCl |
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ020411是一种特异性有效的 PRMT6 抑制剂, IC50 为 10 nM,比作用于 PRMT1 和 PRMT8 的选择性高10倍多。 | |||
T4334 |
EPZ020411 2HCl (1700663-41-7(free base))
|
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ020411 2HCl (1700663-41-7(free base)) 是一种有效且特异性的小分子 PRMT6 抑制剂 (IC50=10 nM)。 | |||
T68378 |
PRMT4-IN-1
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT4-IN-1为PRMT4高选择性抑制剂(IC50=3.2 nM),能有效降低MCF7细胞的相对活力。 |