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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-YL-5092
YL-5092

Chemical Structure : YL-5092

CAS No.: 3056857-07-6

YL-5092 (YL5092)

货号: PC-26021Not For Human Use, Lab Use Only.

YL-5092 is a highly potent and selective, first-in-class inhibitor of RNA m6A reader YTHDC1 with IC50 of 7.4 nM and SPR Kd of 29.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

YL-5092 is a highly potent and selective, first-in-class inhibitor of RNA m6A reader YTHDC1 with IC50 of 7.4 nM and SPR Kd of 29.6 nM.
YL-5092 dose-dependently blocked the binding of substrate mimic, indicating a competitive inhibitor of substrate.
YL-5092 shows no activity against other RNA m6A readers, including YTHDC2, YTHDF1-3, IGF2BP1-3, and HNRNPA2B1.
YL-5092 treatment could dose-dependently stabilize YTHDC1 in MOLM-13 and U937 cells in cellular thermal shift assay (CETSA).
YL-5092 treatment substantially suppressed the proliferation and induced the differentiation and apoptosis of AML cells.
also efficiently inhibited the colony-forming ability of CD34+ AML stem cells, but had no effect on normal hematopoietic stem cells and early progenitors (Lin− Sca1+ Kit+).
YL-5092 treatment impaired leukemogenesis and improved the animal survival rate in mouse AML xenograft models.

物理化学性质&存储条件

分子量 441.43
分子式 C22H14F3N3O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-(Thiazol-5-yl)phenyl)-4-(2-(trifluoromethyl)benzoyl)-1H-pyrrole-2-carboxamide

参考文献

1. Zhang H, et al. Sci Transl Med. 2026 Feb 4;18(835):eadu3137.

2. Shengyong Yang, et al. Discovery of a selective YTHDC1 inhibitor that targets acute myeloid leukemia.

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