WP1066

Catalog No.S2796

WP1066 Chemical Structure

Molecular Weight(MW): 356.22

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. Phase 1.

Size Price Stock Quantity  
In DMSO USD 126 In stock
USD 110 In stock
USD 270 In stock
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4 Customer Reviews

  • Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.

    J Biol Chem 2013 288(36), 26167-76. WP1066 purchased from Selleck.

    (A) HRMECs were treated with IL-6 for 48 hours in the presence and the absence of WP1066. The protein expression and localization of ZO-1 was examined by immunofluorescence staining. Each tight junction protein was doubleimmunostained with anti-CD31 antibody for defining the cell boundaries. Nuclei were labeled with DAPI. Arrow heads indicate the intact tight junction protein at cell boundaries. Scale bars are equal to 50 μm. Right histograms: quantitative analysis of each tight junction protein expression by evaluating the fluorescence intensity using with ImageJ software. The results are fold increases versus control and plotted as the means ± SD (n = 5). * P < 0.05 between two values.

    J Cell Physiol, 2017, 232(5):1123-1134. WP1066 purchased from Selleck.

  • (A) NF-YA, STAT3, pY-STAT3, VEGF and β-actin protein levels were detected by western blot analysis in vector control or NF-YA stably overexpressed (or NF-YA stably overexpressed plus STAT3 inhibitor WP1066 treatment) A375P/Malme-3M cells.

    Oncol Rep, 2016, 35(6):3630-8. WP1066 purchased from Selleck.

    proliferation of GBM6 monolayer and adherent CSC cultures was measured by MTT assay after treatment (72 h) with WP1066 or S3I-201 at the indicated concentrations. 

    WP1066 purchased from Selleck.

Purity & Quality Control

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Biological Activity

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. Phase 1.
Features Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.
Targets
JAK2 [1]
(HEL cells)
STAT3 [2]
(HEL cells)
2.3 μM 2.43 μM
In vitro

WP1066 markedly inhibits the growth of HEL cells carrying the JAK2 V617F mutant isoform in a dose-dependent manner with IC20, IC50 and IC80 of 0.8, 2.3 and 3.8 μM. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM inhibits the phosphorylation of JAK2, STAT3, STAT5, and ERK1/2 without affecting the phosphorylation of JAK1 and JAK3 in erythroid leukemia HEL cells that express the JAK2 V617F isoform. [1] WP1066 at concentrations ranging from 0.5 to 3.0 μM inhibits the proliferation of AML colony-forming cells obtained from patients and that of the AML cell lines OCIM2 and K562 in a dose-dependent manner. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM dose-dependently decreases JAK2 and pJAK2 protein levels as well as downstream phosphorylation levels of STAT3, STAT5, and AKT in OCIM2 and K562 cells. WP1066 at concentrations of 2 μM inhibits OCIM2 cell multiplication by inducing accumulation of cells at the G0-G1 phase of the cell cycle. WP1066 at concentrations of 1, 2, or 3 μM induces apoptosis in both OCIM2 and K562 cells in a dose-dependent fashion by activating procaspase-3 and cleaving PARP. [3] WP1066 at concentrations of 5 μM prevents the phosphorylation of STAT3, and at concentrations of 2.5μM WP1066 significantly inhibits cell survival and proliferation in Caki-1 and 786-O renal cancer cells. WP1066 at concentrations of 5 μM suppresses HIF1α and HIF2α expression and VEGF production in Caki-1 and 786-O renal cancer cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MM1 cells NWXRSHhLTnWwY4Tpc44h[XO|YYm= MVuyOE04OiCq NHjvNYtCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVEh[2WubIOgZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KE2WVDDhd5NigSxiaXO1NF0yNjJizszN M3TrRlIzODN4MkGz
human U266 cells NVqzWpRzTnWwY4Tpc44h[XO|YYm= NX7RUINFOjRvN{KgbC=> M3\EO2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOlYh[2WubIOgZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjVizszN MmjzNlIxOzZ{MUO=
human OCI-My4 cells NFTyS5FHfW6ldHnvckBie3OjeR?= MUSyOE04OiCq MknVRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT1PJMW16PCClZXzsd{Bi\nSncjCyOEB1dyB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwODFOwG0> M3PpVVIzODN4MkGz
human 30M cells M1HRZmN6fG:2b4jpZ:Kh[XO|YYm= NWHHeXJRQCCmYYnz M2PLRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFMxVSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC4JIRigXNiYomgRYxidWG{IFLseYUh[XO|YYmsJGlEPTB;MT64JO69VQ>? MWOyOFkxODZzMh?=
human 73M cells NUnEUYd[S3m2b4TvfIlkyqCjc4PhfS=> M3HkS|gh\GG7cx?= NH[wSXNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckA4O01iY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgPEBl[Xm|IHL5JGFt[W2jcjDCcJVmKGG|c3H5MEBKSzVyPUKuNUDPxE1? NUTJVWd6OjR7MEC2NVI>
human U373MG cells M1q1VGZ2dmO2aX;uJIF{e2G7 NVP6WnhZOjRvN{KgbC=> MkTLRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVUO3N21IKGOnbHzzJIFnfGW{IEK0JJRwKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oy55IN88US=> MWGyNlA{PjJzMx?=
human U87MG cells NVv4d5lLTnWwY4Tpc44h[XO|YYm= NHLWN5czPC15MjDo MVXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOEfNS{Bk\WyuczDh[pRmeiB{NDD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvPiEQvF2= MXuyNlA{PjJzMx?=

... Click to View More Cell Line Experimental Data

In vivo WP1066 orally administrated at dose of 40 mg/kg once daily for 19 days significantly inhibits the tumours growth in Caki-1 xenograft mice, with decreased immunostaining of phosphorylated STAT3 and reduced length of CD34-positive vessels. [4]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: HEL cells carrying the JAK2 V617F mutant isoform, HL60, K562, Raji, PEER, CMK, TM and RHN cells
  • Concentrations: 0 - 6 μM
  • Incubation Time: 72 hours
  • Method: The 3, [4,5-dimethylthiazol-2-yl]-5-[3-carboxymethoxyphenyl]-2-[4-sulfophenyl]-2H-tetrazolium (MTT) assay is done using an MTT-based cell proliferation/cytotoxicity assay system. Briefly, fresh low-density peripheral blood cells and various cell lines at the logarithmic phase of their growth are washed twice in RPMI 1640 containing 10% FCS and counted in a hemocytometer. Cell viability is assessed by the trypan blue (0.1%) staining method. Equal numbers of viable cells (5 × 104 per well) are incubated in a total volume of 100 μL of RPMI 1640 supplemented with 10% FCS alone or with WP1066 at increasing concentrations; the incubations are continued for up to 72 h in 96-well flat-bottomed plates at 37 °C in a humidified 5% CO2 atmosphere. Experiments for each condition are done in triplicate. After incubation, 20 μL of CellTiter96 One Solution Reagent are added to each well. The plates are then incubated for an additional 60 min at 37 °C in a humidified 5% CO2 atmosphere. Immediately after incubation, absorbance is read using a 96-well plate reader at a wavelength of 490 nm.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Caki-1 xenograft mice
  • Formulation: DMSO:polyethylene glycol 300 (20:80)
  • Dosages: 40 mg/kg
  • Administration: Orally administrated
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.31 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.22
Formula

C17H14BrN3O

CAS No. 857064-38-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01904123 Not yet recruiting Brain Cancer|Central Nervous System Neoplasms|Melanoma|Solid Tumors M.D. Anderson Cancer Center|National Institutes of Health (NIH)|National Cancer Institute (NCI) March 2017 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID