WP1066 (WP10666) is a cell permeable AG 490 tyrphostin analog that effectively inhibits the STAT3 pathway. The inhibitor is a potent antitumor agent as displayed in the growth inhibition of malignant glioma cell and acute myelogenous leukemia cells. Stat3
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
CHANNEL BLOCKER, INHIBITOR
Mechanism of action
Channel blocker of K v1.3;Inhibitor of signal transducer and activator of transcription 3
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. A cell permeable inhibitor of Stat3 and JAK2 protein tyrosine kinase.
Associated Targets
STAT3Tchem Signal transducer and activator of transcription 3 0 Activities
1.Ferrajoli A, Faderl S, Van Q, Koch P, Harris D, Liu Z, Hazan-Halevy I, Wang Y, Kantarjian HM, Priebe W et al.. (2007) WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells.. Cancer Res, 67 (23):(11291-9). [PMID:18056455]
2.Verstovsek S, Manshouri T, Quintás-Cardama A, Harris D, Cortes J, Giles FJ, Kantarjian H, Priebe W, Estrov Z. (2008) WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation.. Clin Cancer Res, 14 (3):(788-96). [PMID:18245540]
3.Bill MA, Fuchs JR, Li C, Yui J, Bakan C, Benson Jr DM, Schwartz EB, Abdelhamid D, Lin J, Hoyt DG et al.. (2010) The small molecule curcumin analog FLLL32 induces apoptosis in melanoma cells via STAT3 inhibition and retains the cellular response to cytokines with anti-tumor activity.. Mol Cancer, 9 (3):(165). [PMID:20576164]
4.Tsujita Y, Horiguchi A, Tasaki S, Isono M, Asano T, Ito K, Asano T, Mayumi Y, Kushibiki T. (2017) STAT3 inhibition by WP1066 suppresses the growth and invasiveness of bladder cancer cells.. Oncol Rep, 38 (4):(2197-2204). [PMID:28849140]
5.Li M, Yu H. (2021) Identification of WP1066, an inhibitor of JAK2 and STAT3, as a KV 1.3 potassium channel blocker.. Br J Pharmacol, 178 (13):(2617-2631). [PMID:33689167]
6.Allaf A, Victoria B, Rosario R, Misztal C, Humayun Gultekin S, Dinh CT, Fernandez-Valle C. (2022) WP1066 induces cell death in a schwannomatosis patient-derived schwannoma cell line.. Cold Spring Harb Mol Case Stud, 8 (4):(589-97). [PMID:35732500]
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J2130565