WHI-P154 (Cat.No:I002626) is a promising small molecule inhibitor that has gained attention for its potential therapeutic applications. It specifically targets JAK3 and has shown efficacy in preclinical studies for various autoimmune and inflammatory diseases. Further research is ongoing to explore its clinical benefits and safety profile.
| Catalog Number | I002626 |
| CAS Number | 211555-04-3 |
| Synonyms | 2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol |
| Molecular Formula | C₁₆H₁₄BrN₃O₃ |
| Purity | 95% |
| Target | JAK |
| Solubility | DMSO: ≥ 47 mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 1.8 uM (JAK3); 4 nM(EGFR);100 nM(VEGFR) [1] |
| IUPAC Name | 2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol |
| InChI | InChI=1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20) |
| InChIKey | CBIAKDAYHRWZCU-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)O)Br)OC |
| Reference | </br>1:WHI-P154 enhances the chemotherapeutic effect of anticancer agents in ABCG2-overexpressing cells. Zhang H, Zhang YK, Wang YJ, Kathawala RJ, Patel A, Zhu H, Sodani K, Talele TT, Ambudkar SV, Chen ZS, Fu LW.Cancer Sci. 2014 Aug;105(8):1071-8. doi: 10.1111/cas.12462. Epub 2014 Aug 21. PMID: 24903205 Free PMC Article</br>2:Janus kinase 3 inhibitor WHI-P154 in macrophages activated by bacterial endotoxin: differential effects on the expression of iNOS, COX-2 and TNF-alpha. Sareila O, Korhonen R, Kärpänniemi O, Nieminen R, Kankaanranta H, Moilanen E.Int Immunopharmacol. 2008 Jan;8(1):100-8. Epub 2007 Nov 20. PMID: 18068105 </br>3:JAK inhibitors AG-490 and WHI-P154 decrease IFN-gamma-induced iNOS expression and NO production in macrophages. Sareila O, Korhonen R, Kärpänniemi O, Nieminen R, Kankaanranta H, Moilanen E.Mediators Inflamm. 2006;2006(2):16161. PMID: 16883061 Free PMC Article</br>4:The JAK3 inhibitor WHI-P154 prevents PDGF-evoked process outgrowth in human neural precursor cells. Richards GR, Smith AJ, Cuddon P, Ma QP, Leveridge M, Kerby J, Roderick HL, Bootman MD, Simpson PB.J Neurochem. 2006 Apr;97(1):201-10. Epub 2006 Mar 3. PMID: 16515549 Free Article</br>5:Inhibition of the antigen-induced activation of rodent mast cells by putative Janus kinase 3 inhibitors WHI-P131 and WHI-P154 in a Janus kinase 3-independent manner. Linwong W, Hirasawa N, Aoyama S, Hamada H, Saito T, Ohuchi K.Br J Pharmacol. 2005 Jul;145(6):818-28. PMID: 15852029 Free PMC Article</br>6:Inhibition of human glioblastoma cell adhesion and invasion by 4-(4/’-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3/’-bromo-4/’-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154). Narla RK, Liu XP, Klis D, Uckun FM.Clin Cancer Res. 1998 Oct;4(10):2463-71. PMID: 9796979 Free Article |
