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573097

Sigma-Aldrich

STAT3 Inhibitor III, WP1066

STAT3 Inhibitor III, WP1066, CAS 857064-38-1, is a cell-permeable AG490 tyrphostin analog that acts as a STAT3 pathway inhibitor. A potent anti-tumor agent.

Synonym(s):

STAT3 Inhibitor III, WP1066

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About This Item

Empirical Formula (Hill Notation):
C17H14BrN3O
CAS Number:
Molecular Weight:
356.22
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 10 mg/mL
ethanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

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

InChI key

VFUAJMPDXIRPKO-LQELWAHVSA-N

General description

A cell-permeable AG 490 (Cat. No. 658401) tyrphostin analog that acts as an effective STAT3 pathway inhibitor and a much more potent antitumor agent than AG 490 in inhibiting malignant glioma growth both in cultures in vitro (IC50 = 5.6 and 3.7 µM in a viability assay using U87-MG and U373-MG, respectively; no inhibition against nontumor NHA at 10 µM) and in mice in vivo. Shown to cross blood-brain barrier in mice in vivo. Also available in InSolution format (Cat. No. 573129.
A cell-permeable AG 490 (Cat. No. 658401) tyrphostin analog that acts as an effective STAT3 pathway inhibitor and a much more potent antitumor agent than AG 490 in inhibiting malignant glioma growth both in cultures in vitro (IC50 = 5.6 and 3.7 µM in a viability assay using U87-MG and U373-MG, respectively; no inhibition against nontumor NHA at 10 µM) and in mice in vivo. Shown to cross blood-brain barrier in mice in vivo.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
STAT3 pathway
Product does not compete with ATP.
Reversible: no
Target IC50: 5.6 and 3.7 µM in inhibiting malignant glioma growth in a viability assay using U87-MG and U373-MG, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Iwamaru, A., et al. 2007. Oncogene,26, 2435.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Alicia Haydo et al.
EMBO reports, 24(12), e56964-e56964 (2023-11-08)
Glioblastoma is a very aggressive tumor and represents the most common primary brain malignancy. Key characteristics include its high resistance against conventional treatments, such as radio- and chemotherapy and its diffuse tissue infiltration, preventing complete surgical resection. The analysis of
In-Hye Ham et al.
International journal of oncology, 61(1) (2022-05-28)
The present study aimed to investigate whether the Janus‑activated kinase (JAK)/signal transducer and activator of transcription 3 (STAT3) signaling pathway is a critical mechanism underlying the cancer‑associated fibroblast (CAF)‑induced chemoresistance of gastric cancer (GC). In addition, the present study tried to
Meng Chi et al.
Annals of translational medicine, 8(8), 531-531 (2020-05-16)
Dexmedetomidine (DEX), a highly selective α2-adrenergic receptor agonist, has been reported to increase the malignancy of breast cancer cells in vitro and stimulate tumor growth in mice. Transmembrane protease serine 2 (TMPRSS2) demonstrates proteolytic activity, resulting in degradation of the
Eun-Ji Lim et al.
Cell death & disease, 13(4), 417-417 (2022-04-30)
Colorectal cancer (CRC) has a 5-year survival rate of <10%, as it can metastasize to the lungs and liver. Anticancer drugs and targeted therapies used to treat metastatic colorectal cancer have insufficient therapeutic efficacy and are associated with complications. Therefore
Ahmad Sharanek et al.
Cell reports, 36(9), 109647-109647 (2021-09-02)
Brain tumor stem cells (BTSCs) and intratumoral heterogeneity represent major challenges in glioblastoma therapy. Here, we report that the LGALS1 gene, encoding the carbohydrate binding protein, galectin1, is a key regulator of BTSCs and glioblastoma resistance to therapy. Genetic deletion

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