WDR5-IN-1
- CAS No.
- 2408842-51-1
- Chemical Name:
- WDR5-IN-1
- Synonyms
- WDR5-IN-1;WDR-5-IN-1,WDR5 IN 1,WDR5IN1;1(2H)-Isoquinolinone, 7-[(2,3-dihydro-2-imino-3-methyl-1H-imidazol-1-yl)methyl]-2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-3,4-dihydro-
- CBNumber:
- CB28054577
- Molecular Formula:
- C30H31FN4O3
- Molecular Weight:
- 514.59
- MDL Number:
- MFCD34469869
- MOL File:
- 2408842-51-1.mol
WDR5-IN-1 Chemical Properties,Uses,Production
Biological Activity
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].
References
[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.
WDR5-IN-1 Preparation Products And Raw materials
Raw materials
Preparation Products
WDR5-IN-1 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
| Shaanxi kelkai Pharmaceutical Technology Co., Ltd | 029-2148545164 17392779578 | 2148545164@qq.com | China | 6807 | 58 |
| RD International Technology Co., Limited | 18988968278 | sales@ubiochem.com | China | 9146 | 58 |