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Cat. No. Product Name Target Signaling Pathways
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).
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。
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。
T61986 PRMT5-IN-21

PRMT5-IN-21 (compound 1) 是有效的环核苷PRMT5抑制剂。
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。
T76413 PRMT5-IN-22

PRMT5-IN-22(compound 53)是一种针对蛋白精氨酸甲基转移酶5PRMT5)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。
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].
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。
T39008 PRMT5-IN-4

PRMT5-IN-4

PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor.
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。
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。
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...
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。
T79873 TNG-462

Histone Methyltransferase Chromatin/Epigenetic
TNG-462(化合物1143)作为一种口服有效的PRMT5抑制剂,适用于研究MTAP缺失型及/或MTA累积型癌症。

化合物

PRMT5-IN-1
Cat.No: T12541
Synonym:
Target: Histone Methyltransferase
PRMT5-IN-1 hydrochloride
Cat.No: T62815
Synonym:
Target:
PRMT5-IN-29
Cat.No: T78172
Synonym:
Target: Histone Methyltransferase
PRMT5-IN-21
Cat.No: T61986
Synonym:
Target:
PRMT5-IN-23
Cat.No: T76414
Synonym:
Target:
PRMT5-IN-22
Cat.No: T76413
Synonym:
Target:
PRMT5-IN-19
Cat.No: T61862
Synonym:
Target:
PRMT5-IN-28
Cat.No: T79035
Synonym:
Target: Histone Methyltransferase
PRMT5-IN-4
Cat.No: T39008
Synonym: PRMT5-IN-4
Target:
PRMT5-IN-31
Cat.No: T79274
Synonym:
Target: Histone Methyltransferase
PRMT5-IN-25
Cat.No: T78152
Synonym:
Target: Histone Methyltransferase
MRTX9768 hydrochloride
Cat.No: T36630
Synonym:
Target:
Antiproliferative agent-25
Cat.No: T79275
Synonym:
Target: Histone Methyltransferase
TNG-462
Cat.No: T79873
Synonym:
Target: Histone Methyltransferase
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