Date published: 2025-11-9

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Stat3 Inhibitor III, WP1066 (CAS 857064-38-1)

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Alternate Names:
(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide
Application:
Stat3 Inhibitor III, WP1066 is a cell permeable inhibitor of Stat3 and JAK2 protein tyrosine kinase
CAS Number:
857064-38-1
Purity:
≥97%
Molecular Weight:
356.2
Molecular Formula:
C17H14BrN3O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Stat3 inhibitor III, 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 Inhibitor III, WP1066 has shown more potency as an antitumor agent than AG 490 (sc-202046) when inhibiting malignant glioma growth in vitro. Stat3 inhibitor III, WP1066 also acts as an immune adjuvant by inducing proliferation of effector T cells and upregulating CD86 and CD80. In addition Stat3 inhibitor III, WP1066 has displayed inhibition of JAK2 protein tyrosine kinase as well as suggested activation of Bax.


Stat3 Inhibitor III, WP1066 (CAS 857064-38-1) References

  1. A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo.  |  Iwamaru, A., et al. 2007. Oncogene. 26: 2435-44. PMID: 17043651
  2. A novel small molecule inhibitor of signal transducers and activators of transcription 3 reverses immune tolerance in malignant glioma patients.  |  Hussain, SF., et al. 2007. Cancer Res. 67: 9630-6. PMID: 17942891
  3. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells.  |  Ferrajoli, A., et al. 2007. Cancer Res. 67: 11291-9. PMID: 18056455
  4. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation.  |  Verstovsek, S., et al. 2008. Clin Cancer Res. 14: 788-96. PMID: 18245540
  5. Leptin attenuates cardiac apoptosis after chronic ischaemic injury.  |  McGaffin, KR., et al. 2009. Cardiovasc Res. 83: 313-24. PMID: 19233863
  6. STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma.  |  Horiguchi, A., et al. 2010. Br J Cancer. 102: 1592-9. PMID: 20461084
  7. The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models.  |  Hatiboglu, MA., et al. 2012. Int J Cancer. 131: 8-17. PMID: 21792892
  8. STAT3 inhibitor WP1066 as a novel therapeutic agent for bCCI neuropathic pain rats.  |  Xue, ZJ., et al. 2014. Brain Res. 1583: 79-88. PMID: 25084036
  9. WP1066 sensitizes oral squamous cell carcinoma cells to cisplatin by targeting STAT3/miR-21 axis.  |  Zhou, X., et al. 2014. Sci Rep. 4: 7461. PMID: 25514838
  10. The STAT3 inhibitor WP1066 reverses the resistance of chronic lymphocytic leukemia cells to histone deacetylase inhibitors induced by interleukin-6.  |  Lu, K., et al. 2015. Cancer Lett. 359: 250-8. PMID: 25636517
  11. The STAT3 inhibitor WP1066 synergizes with vorinostat to induce apoptosis of mantle cell lymphoma cells.  |  Lu, K., et al. 2015. Biochem Biophys Res Commun. 464: 292-8. PMID: 26116769
  12. WP1066 suppresses macrophage cell death induced by inflammasome agonists independently of its inhibitory effect on STAT3.  |  Honda, S., et al. 2017. Cancer Sci. 108: 520-527. PMID: 28035720
  13. STAT3 inhibition by WP1066 suppresses the growth and invasiveness of bladder cancer cells.  |  Tsujita, Y., et al. 2017. Oncol Rep. 38: 2197-2204. PMID: 28849140
  14. Stat3/Oct-4/c-Myc signal circuit for regulating stemness-mediated doxorubicin resistance of triple-negative breast cancer cells and inhibitory effects of WP1066.  |  Cheng, CC., et al. 2018. Int J Oncol. 53: 339-348. PMID: 29750424

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Stat3 Inhibitor III, WP1066, 10 mg

sc-203282
10 mg
$132.00

how to diluted the inhibitor and how about the work concentration for cell?where can I download the protocol of the inhibitor,thanks very much!

Asked by: ting chen
Thank you for the question. We suggest diluting the solid product in DMSO or EtOH. You might want to check the available background references for this compound listed below. Please contact our Technical Service Dept. if you have further questions. 1. Hussain, S.F., et al. 2007. Cancer Res. 67: 9630-9636. PMID: 17942891 2. Ferrajoli, A., et al. 2007. Cancer Res. 67: 11291-11299. PMID: 18056455 3. Iwamaru, A., et al. 2007. Oncogene. 26: 2435-2444. PMID: 17043651 4. McGaffin, K.R., et al. 2009. Cardiovasc. Res. 83: 313-324. PMID: 19233863
Answered by: Technical Support Europe
Date published: 2022-11-14

What are the recommended storage conditions (if any) once the product is in solution?

Asked by: 13punMA
Thank you for your question about our product Stat3 Inhibitor III, WP1066 (CAS# 857064-38-1) We recommend storing storing the product in powder form in -20℃; if the product is in solvent for 6 months at -80℃.
Answered by: Chemical Support 8
Date published: 2022-11-14
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Rated 5 out of 5 by from ReitsmaReitsma, J.M. et al. (PubMed 23903834) used product sc-203282 (Stat3 Inhibitor III, WP1066), a known STAT3 and JAK-2 inhibitor, to determine if disruption of JAK signaling would prevent human CMV (HCMV)-mediated nuclear localization of STAT3 or disrupt viral DNA replication. While sc-203282 was successful in disrupting JAK signaling, it was unable to disrupt viral replication or prevent nuclear localization of STAT3. -SCBT Publication Review
Date published: 2015-02-26
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Stat3 Inhibitor III, WP1066 is rated 5.0 out of 5 by 1.
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