Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T39809 |
PRMT5-IN-14
PRMT5-IN-14 |
||
PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations. | |||
T40313 |
PRMT5-IN-9
PRMT5-IN-9 |
||
PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC 50 of 0.01 μM. | |||
T39993 |
PRMT5-IN-15
PRMT5-IN-15 |
||
PRMT5-IN-15 is a PRMT5 inhibitor with an IC 50 value of 0.84 nM. | |||
T40202 |
PRMT5-IN-12
PRMT5-IN-12 |
||
PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5 . | |||
T40197 |
PRMT5-IN-11
PRMT5-IN-11 |
||
PRMT5-IN-11 demonstrates potent structure-dependent inhibition against the protein methyltransferase PRMT5:MEP50 complex at submicromolar concentrations. | |||
T39008 |
PRMT5-IN-4
PRMT5-IN-4 |
||
PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor. | |||
T39934 |
PRMT5-IN-13
PRMT5-IN-13 |
||
PRMT5-IN-13 is a selective inhibitor of protein arginine methyltransferase 5 (prmt5) . | |||
T16577 |
PRMT5-IN-2
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5. | |||
T12541 | PRMT5-IN-1 | Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50). | |||
T72785 |
PRMT5:MEP50 PPI
|
||
PRMT5:MEP50 PPI是一款新型的抑制剂,专门针对PRMT5:MEP50蛋白-蛋白相互作用,展现了抗肿瘤活性,并对肺癌及前列腺癌细胞具有显著的抗增殖效果。 | |||
T40254 |
MRTX-1719
|
Histone Methyltransferase | Chromatin/Epigenetic |
MRTX-1719 是有效的PRMT5/MTA 复合体选择性抑制剂,其对PRMT5/MTAMTAPDELSDMA 细胞系的IC50值为 <10 nM。 | |||
T63860 |
PRMT5-IN-18
|
||
PRMT5-IN-18 (Compound 002) 是 PRMT5 的有效抑制剂,能够用于由 PRMT5 介导的疾病(如肿瘤)的研究。 | |||
T78172 |
PRMT5-IN-29
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-29,一种有效的口服活性PRMT5抑制剂,IC50值为1.5 μΜ,具潜力用于晚期癌症研究。 | |||
T63103 | PRMT5-IN-17 | ||
PRMT5-IN-17 (Compound 6) 是一种 PRMT5 抑制剂,表现出抗肿瘤活性。其中 PRMT5 是一种蛋白质精氨酸甲基转移酶,是新型的与表观遗传修饰相关的抗肿瘤靶点。 | |||
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]. | |||
T78152 |
PRMT5-IN-25
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-25(化合物503)是一种高效的PRMT5抑制剂,具有0.06 nM的Ki值,并展现出抗增殖活性。 | |||
T61986 | PRMT5-IN-21 | ||
PRMT5-IN-21 (compound 1) 是有效的环核苷PRMT5抑制剂。 | |||
T62683 | PRMT5-IN-3 | ||
PRMT5-IN-3 是一种 PRMT5 抑制剂。PRMT5-IN-3 联合 DNA 损伤剂,对肿瘤细胞具有合成致死性。 | |||
T76413 | PRMT5-IN-22 | ||
PRMT5-IN-22(compound 53)是一种针对蛋白精氨酸甲基转移酶5(PRMT5)的选择性抑制剂,显示出抗肿瘤活性。PRMT5作为表观遗传修饰中的新型抗肿瘤靶点,属于蛋白质精氨酸甲基转移酶类。 | |||
T79274 |
PRMT5-IN-31
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-31(Compound 3m)作为一种高选择性PRMT5抑制剂,其IC50为0.31 μM。它能够通过占据PRMT5的底物位点以及与氨基酸残基形成必要相互作用来上调hnRNP E1蛋白水平。此外,PRMT5-IN-31能有效抑制A549细胞增殖,其机制涉及诱导apoptosis和阻碍细胞迁移。该化合物在人肝微粒体中表现出较高的代谢稳定性,半衰期为132.4分钟。 | |||
T69430 |
PRMT5-IN-C17
|
||
PRMT5-IN-C17 is a novel potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor. | |||
T60725 |
PRMT5-IN-10
|
||
PRMT5-IN-10 对蛋白甲基转移酶 PRMT5:MEP50复合物表现出良好的结构依赖性抑制作用。 | |||
T63138 |
PRMT5-IN-16
|
||
PRMT5-IN-16 (Compound 20) 是一种 PRMT5 抑制剂,具有抗肿瘤作用。其中 PRMT5 是一种蛋白质精氨酸甲基转移酶,是新型的与表观遗传修饰相关的抗肿瘤靶点。 | |||
T76414 |
PRMT5-IN-23
|
||
PRMT5-IN-23(compound 50)是一种针对蛋白精氨酸甲基转移酶5 (PRMT5) 的选择性抑制剂,展现出抗肿瘤活性。作为一种与表观遗传修饰相关的靶点,PRMT5在新型抗肿瘤疗法中具有重要地位。 | |||
T79035 |
PRMT5-IN-28
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-28(化合物36)是一种PRMT5抑制剂,能够调控包含基因转录、mRNA剪接、DNA修复、蛋白质定位、细胞命运和信号传导等过程的蛋白质精氨酸甲基化。PRMT5的异常活性与癌症细胞的增殖、抗凋亡、侵袭转移能力增强及免疫逃逸机制的影响相关。 | |||
T62815 | PRMT5-IN-1 hydrochloride | ||
PRMT5 IN-1 hydrochloride (compound 9) 是一种半缩醛胺,是一种选择性蛋白精氨酸甲基转移酶5 (PRMT5) 的有效抑制剂,对 PRMT5/MEP50 具有抑制作用 (IC50: 11 nM)。PRMT5 IN-1 hydrochloride 在生理条件下可以转化为醛,并与 C449 反应,形成共价加合物。 | |||
T9575 |
MRTX9768
|
Histone Methyltransferase | Chromatin/Epigenetic |
MRTX-9768 是一种有效的、选择性的、具有口服活性的 PRMT5-MTA 复合体抑制剂,可选择性靶向 MTAP/CDKN2A 缺失的肿瘤。 | |||
T14141 |
AGI-24512
|
Others; Methionine Adenosyltransferase (MAT) | Chromatin/Epigenetic; Others |
AGI-24512 是一种甲硫氨酸腺苷转移酶 2A 抑制剂,在体外能够阻断 MTAP 缺失的癌细胞的生长,可用于研究癌症。 | |||
T15767 |
LLY-283
|
Histone Methyltransferase | Chromatin/Epigenetic |
LLY-283 是一种有效的,选择性的,可口服的蛋白精氨酸甲基转移酶 5 (PRMT5) 抑制剂,对 PRMT5:MEP50 复合物的作用很强,IC50 和 Kd 值分别为 22 nM 和 6 nM,具有抗肿瘤活性。 | |||
T6853 |
GSK591
GSK3203591,EPZ015866 |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK591 (GSK3203591) 是一种有效的精氨酸甲基转移酶 PRMT5 选择性抑制剂,IC50值为 11 nM。 | |||
T6857 |
HLCL-61 hydrochloride
HLCL61,HLCL-61 HCL |
Apoptosis; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
HLCL-61 hydrochloride (HLCL-61 HCL) 是小分子蛋白精氨酸甲基转移酶 5 抑制剂。 | |||
T6076 |
EPZ015666
GSK3235025 |
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ015666 (GSK3235025) 是一种口服有效的 PRMT5 酶活性抑制剂,IC50为 22 nM。 | |||
T9329 |
BRD0639
|
Histone Methyltransferase | Chromatin/Epigenetic |
BRD0639 是首创的PRMT5-substrate adaptor interaction 的抑制剂。BRD0639 是一种 PRMT5 结合基序 (PBM) 竞争性抑制剂,可以支持 PBM 依赖的 PRMT5 活性的研究。 | |||
T10850 |
CMP-5
|
Antiviral; Histone Methyltransferase | Chromatin/Epigenetic; Immunology/Inflammation |
CMP-5 是一种具有选择性的 PRMT5 抑制剂,是刺突蛋白、神经纤毛蛋白受体和 ACE2 的强结合剂,抑制 PRMT5 甲基转移酶活性。CMP-5 具有抗病毒活性,可用于研究SARS病毒感染。 | |||
T5745 |
GSK3326595
EPZ015938 |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK3326595 (EPZ015938) 是一种选择性可逆的蛋白精氨酸甲基转移酶 5 抑制剂,IC50为6.2 nM,具有广谱的抗增殖活性。 | |||
T73494 |
TNG908
|
||
TNG908 是一种可通过血脑屏障的 MTAP-协同PRMT5抑制剂,TNG908 对 MTAP 细胞系的选择性比 MTAPWT 细胞系高 15倍,可用于癌症研究。 | |||
T67947 |
WDR5-0102
|
Histone Methyltransferase | Chromatin/Epigenetic |
WDR5-0102为针对WDR5-MLL1的抑制剂(Kdis=7 μM, Kd=4 μM)。该化合物有效抑制MLL1活性,而对人类H3K4甲基转移酶SETD7及其他六种HMT(G9a、EHMT1、SUV39H2、SETD8、PRMT3、PRMT5)不表现出抑制作用。 | |||
T11131 |
DW14800
|
Histone Methyltransferase | Chromatin/Epigenetic |
DW14800是PRMT5的抑制剂(IC50 = 17 nM),能增强HNF4α的转录,并降低H4R3me2s 的水平。 | |||
T40233 |
(Iso)-MS4322
(Iso)-YS43-22,MS4322 (isomer),YS43-22 (isomer) |
Histone Methyltransferase | Chromatin/Epigenetic |
(Iso)-MS4322 ((Iso)-YS43-22) 是一种具有选择性和强效性的蛋白质精氨酸甲基转移酶 5 (PRMT5) 降解剂,具有潜在的抗癌活性,有效地降低 MCF-7 细胞中的 PRMT5 蛋白水平,可抑制多种癌细胞的生长。 | |||
T15624 |
JNJ-64619178
|
Histone Methyltransferase | Chromatin/Epigenetic |
JNJ-64619178 是一种选择性的、口服活性的、假不可逆的蛋白质精氨酸甲基转移酶 5 抑制剂,IC50为 0.14 nM,有用于肺癌的研究潜力。 | |||
T26836 | BLL5 Maleate | ||
BLL5 Maleate is a first-in-class selective PRMT5 inhibitor, it blocks EBV-driven B lymphocyte transformation and survival while leaving normal B cells unaffected. | |||
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. | |||
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. | |||
T79275 |
Antiproliferative agent-25
|
Histone Methyltransferase | Chromatin/Epigenetic |
Antiproliferative agent-25 (Compound 3s4)作为一种选择性PRMT5抑制剂(IC50: 0.11 μM),能够上调hnRNP E1蛋白水平,并通过与SAM及PRMT5的E444残基形成氢键相互作用。该化合物通过促进apoptosis和抑制细胞迁移,有效抑制A549细胞的增殖。此外,Antiproliferative agent-25在人和大鼠肝微粒体中的高清除率表明,其T1/2分别为21.8和4.7分钟。 | |||
T28448 |
PR5-LL-CM01
|
||
PR5-LL-CM01 is a novel protein arginine methyltransferase 5 (PRMT5) inhibitor in colorectal and pancreatic cancers. | |||
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. | |||
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 ... | |||
T71767 |
WX2-43
|
||
WX2-43 is a Novel potent PRMT5 specific inhibitor, specifically blocking KLF4-mediated transcription and cell survival, suppressing breast tumor progression. | |||
T36630 | MRTX9768 hydrochloride | ||
MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-de... | |||
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. |