Catalog No.S2796

For research use only.

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. WP1066 induces apoptosis. Phase 1.

WP1066 Chemical Structure

CAS No. 857064-38-1

Selleck's WP1066 has been cited by 58 publications

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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. WP1066 induces apoptosis. Phase 1.
Features Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.
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 M4K1OmZ2dmO2aX;uJIF{e2G7 Mlm2NlQuPzJiaB?= NG[2cIlCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVEh[2WubIOgZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KE2WVDDhd5NigSxiaXO1NF0yNjJizszN NF\mWFkzOjB|NkKxNy=>
human U266 cells NY\tU4RqTnWwY4Tpc44h[XO|YYm= NF\IfZAzPC15MjDo M4q2VGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOlYh[2WubIOgZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjVizszN MYSyNlA{PjJzMx?=
human OCI-My4 cells M3rJN2Z2dmO2aX;uJIF{e2G7 NYHFOnV6OjRvN{KgbC=> MkPnRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT1PJMW16PCClZXzsd{Bi\nSncjCyOEB1dyB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwODFOwG0> MVWyNlA{PjJzMx?=
human 30M cells NVzRWGxIS3m2b4TvfIlkyqCjc4PhfS=> MlHFPEBl[Xm| MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCzNG0h[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiODDkZZl{KGK7IFHsZY1ieiCEbIXlJIF{e2G7LDDJR|UxRTFwODFOwG0> NE\kU2gzPDlyME[xNi=>
human 73M cells NXzGeYpbS3m2b4TvfIlkyqCjc4PhfS=> MYO4JIRigXN? NHf2eHhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckA4O01iY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgPEBl[Xm|IHL5JGFt[W2jcjDCcJVmKGG|c3H5MEBKSzVyPUKuNUDPxE1? NWDwb2JROjR7MEC2NVI>
human U373MG cells MXXGeY5kfGmxbjDhd5NigQ>? M120blI1NTd{IHi= MXXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXM{ezUWch[2WubIOgZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0{NjdizszN NXHjRYJPOjJyM{[yNVM>
human U87MG cells M3\pR2Z2dmO2aX;uJIF{e2G7 MnHLNlQuPzJiaB?= M2fRSGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGW4O21IKGOnbHzzJIFnfGW{IEK0JJRwKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS54IN88US=> NE\jc5QzOjB|NkKxNy=>
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-ERK / ERK 20461084
Cell viability Cell viability 28496056
Immunofluorescence N-cadherin / E-cadherin / Vimentin / β-catenin 26690371
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 (from reference)

Cell Research:[1]
  • 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.
Animal Research:[4]
  • Animal Models: Caki-1 xenograft mice
  • Dosages: 40 mg/kg
  • Administration: Orally administrated

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 356.22


CAS No. 857064-38-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04334863 Recruiting Drug: WP1066 Brain Tumor|Medulloblastoma|Brain Metastases Emory University|CURE Childhood Cancer Inc.|Peach Bowl LegACy Fund May 4 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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