WP1066

• CAT Number: I005146
• CAS Number: 857064-38-1
• Molecular Formula: C₁₇H₁₄BrN₃O
• Molecular Weight: 356.22
• Purity: ≥95%
• Target: JAK
• Solubility: DMSO: ≥ 44 mg/mL
• Storage: 3 years -20C powder
• IC50: 2.3/2.43 uM (JAK2/STAT3) [1] [2]
• InChI: InChI=1S/C17H14BrN3O/c1-12(13-6-3-2-4-7-13)20-17(22)14(11-19)10-15-8-5-9-16(18)21-15/h2-10,12H,1H3,(H,20,22)/b14-10+/t12-/m0/s1
• InChIKey: VFUAJMPDXIRPKO-LQELWAHVSA-N
• SMILES: CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

WP1066 (CAT: I005146) is a small-molecule inhibitor that exerts its pharmacologic action by targeting multiple signaling pathways, including signal transducer and activator of transcription 3 (STAT3), Janus kinase 2 (JAK2), and histone deacetylases (HDACs). By inhibiting STAT3 activation, WP1066 hinders cancer cell growth and survival. Its ability to target JAK2 and HDACs further contributes to its anti-cancer and anti-inflammatory effects. WP1066 shows promise as a potential therapeutic agent for various cancers, including glioblastoma, multiple myeloma, and breast cancer. It represents a valuable tool for targeting STAT3-driven pathways in cancer and inflammation-related conditions.

Reference

1:WP1066 suppresses macrophage cell death induced by inflammasome agonists independently of its inhibitory effect on STAT3. Honda S, Sadatomi D, Yamamura Y, Nakashioya K, Tanimura S, Takeda K.Cancer Sci. 2017 Mar;108(3):520-527. doi: 10.1111/cas.13154. PMID: 28035720 Free PMC Article2:WP1066 exhibits antitumor efficacy in nasal‑type natural killer/T-cell lymphoma cells through downregulation of the STAT3 signaling pathway. Geng L, Li X, Zhou X, Fang X, Yuan D, Wang X.Oncol Rep. 2016 Nov;36(5):2868-2874. doi: 10.3892/or.2016.5091. Epub 2016 Sep 15. PMID: 27633398 3:Delayed Administration of WP1066, an STAT3 Inhibitor, Ameliorates Radiation-Induced Lung Injury in Mice. Yu J, Yuan X, Liu Y, Zhang K, Wang J, Zhang H, Liu F.Lung. 2016 Feb;194(1):67-74. doi: 10.1007/s00408-015-9821-8. Epub 2015 Nov 13. PMID: 26563331 4:The STAT3 inhibitor WP1066 synergizes with vorinostat to induce apoptosis of mantle cell lymphoma cells. Lu K, Chen N, Zhou XX, Ge XL, Feng LL, Li PP, Li XY, Geng LY, Wang X.Biochem Biophys Res Commun. 2015 Aug 14;464(1):292-8. doi: 10.1016/j.bbrc.2015.06.145. Epub 2015 Jun 24. PMID: 26116769 5:The STAT3 inhibitor WP1066 reverses the resistance of chronic lymphocytic leukemia cells to histone deacetylase inhibitors induced by interleukin-6. Lu K, Fang XS, Feng LL, Jiang YJ, Zhou XX, Liu X, Li PP, Chen N, Ding M, Wang N, Zhang J, Wang X.Cancer Lett. 2015 Apr 10;359(2):250-8. doi: 10.1016/j.canlet.2015.01.021. Epub 2015 Jan 27. PMID: 25636517 6:WP1066 sensitizes oral squamous cell carcinoma cells to cisplatin by targeting STAT3/miR-21 axis. Zhou X, Ren Y, Liu A, Jin R, Jiang Q, Huang Y, Kong L, Wang X, Zhang L.Sci Rep. 2014 Dec 17;4:7461. doi: 10.1038/srep07461. PMID: 25514838 Free PMC Article7:STAT3 inhibitor WP1066 as a novel therapeutic agent for bCCI neuropathic pain rats. Xue ZJ, Shen L, Wang ZY, Hui SY, Huang YG, Ma C.Brain Res. 2014 Oct 2;1583:79-88. doi: 10.1016/j.brainres.2014.07.015. Epub 2014 Jul 30. PMID: 25084036 8:[Signal transducer and activator of transcription-3 inhibitor WP1066 affects human tongue squamous cell carcinoma proliferation and apoptosis in vitro and in vivo]. Huang Y, Zhou X, Liu A, Li S, Wang X, Zhang L.Zhonghua Kou Qiang Yi Xue Za Zhi. 2014 May;49(5):308-13. Chinese. PMID: 25031007 9:STAT3 inhibitor WP1066 attenuates miRNA-21 to suppress human oral squamous cell carcinoma growth in vitro and in vivo. Zhou X, Ren Y, Liu A, Han L, Zhang K, Li S, Li P, Li P, Kang C, Wang X, Zhang L.Oncol Rep. 2014 May;31(5):2173-80. doi: 10.3892/or.2014.3114. Epub 2014 Mar 27. PMID: 24676554 10:The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models. Hatiboglu MA, Kong LY, Wei J, Wang Y, McEnery KA, Fuller GN, Qiao W, Davies MA, Priebe W, Heimberger AB.Int J Cancer. 2012 Jul 1;131(1):8-17. doi: 10.1002/ijc.26307. Epub 2011 Aug 24. PMID: 21792892 Free PMC Article