WDR5-IN-1 |
| Catalog No.GC62558 |
WDR5-IN-1은 Kd가 <0.02nM인 강력하고 선택적인 WD 반복 도메인 5(WDR5) 억제제입니다. WDR5-IN-1은 2.2nM의 IC50으로 MLL1 히스톤 메틸트랜스퍼라제(HMT) 활성을 억제합니다. WDR5-IN-1은 WDR5 치환 유전자에서 MYC 모집을 감소시키고 CHP-134(신경모세포종) 및 라모스(버킷 림프종) 계통에서 강력한 항증식 효과를 나타냅니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2408842-51-1
Sample solution is provided at 25 µL, 10mM.
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WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].
WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1].WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1].WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM[1].
[1]. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675.
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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