WP1066

Name: WP1066
Brand: MedChemExpress
SKU: HY-15312
Rating: 5.0 (29 reviews)

Cat. No.: HY-15312 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

For research use only. We do not sell to patients.

WP1066 Chemical Structure

CAS No. : 857064-38-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 62	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 62	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 57	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 277	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 29 publication(s) in Google Scholar

25 Publications Citing Use of MCE WP1066

: WP1066 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Feb;41(2):218-228. [Abstract]; HUVECs are pretreated with WP1066 for 1 h, followed by ZYZ-803 (1 μM) for 30 min. Protein levels are assessed by Western blot.

: WP1066 purchased from MedChemExpress. Usage Cited in: Cancer Manag Res. 2018 Nov 26;10:6339-6355. [Abstract]; Western blotting analysis: treatment with the Stat3 inhibitor WP1066 neutralizes the up-regulation of MMP2 and MMP9 and reverses the EMT progression caused by the overexpression of Uck2 in Bel-7402 cells.

: WP1066 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2017 Apr 17;108:542-553. [Abstract]; The role of STAT3 in SERPINB1-mediated protecting ALI in OALT is further confirmed by using STAT3 specific inhibitor WP1066. post-OALT lung STAT3 activation is significantly increased evidenced by elevated phosphorylation of STAT3 at site727 and site705 (P<0.01 vs sham), which are associated with enhanced HO-1 protein expression.

: WP1066 purchased from MedChemExpress. Usage Cited in: J Cancer. 2017 Feb 25;8(5):816-824. [Abstract]; The protein expression levels of p-Akt, t-Akt, p-STAT3, t-STAT3, MMP2 and MMP9 are determined via western blotting 48 h after knockdown of B7-H3 and blockade of the PI3K/Akt pathway using LY294002 or the STAT3 pathway using WP1066.

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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

IC₅₀ & Target^[1]^[2]

JAK2

STAT3

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	4.2 μM Compound: WP1066	Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34055214]
U-266	IC₅₀	1.5 μM Compound: WP1066	Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-373MG ATCC	IC₅₀	3.7 μM Compound: WP1066	Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]
U-87MG ATCC	IC₅₀	5.6 μM Compound: WP1066	Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay	[PMID: 22036213]

In Vitro

WP1066 markedly inhibits the growth of HEL cells in a dose-dependent manner. The IC₅₀ value for inhibition of the proliferation of HEL cells is 2.3 μM. WP1066 inhibits the growth of human HEL cells carrying the JAK2 V617F mutant isoform^[1]. Blockade of p-STAT3 with WP1066 enhances the cytotoxic effects of CTX on the tumor. The IC₅₀ doses of WP1066 for B16 cells is 2.43 μM (0.865 μg/mL)^[2]. WP1066 inhibits AML blast colony-forming cell proliferation, suppresses normal BM progenitor proliferation at increased concentrations, and inhibits AML colony-forming cell proliferation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

WP1066 (30 mg/kg, o.g.) exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

356.22

Formula

C₁₇H₁₄BrN₃O

CAS No.

857064-38-1

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N[C@H](C1=CC=CC=C1)C)/C(C#N)=C/C2=NC(Br)=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 44 mg/mL (123.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 16.67 mg/mL (46.80 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8073 mL	14.0363 mL	28.0725 mL
5 mM	0.5615 mL	2.8073 mL	5.6145 mL
10 mM	0.2807 mL	1.4036 mL	2.8073 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Verstovsek S, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res, 2008, (3), 788-796. [Content Brief]

[2]. Hatiboglu MA, et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of WP1066 in murine melanoma models. Int J Cancer, 2012, 131(1), 8-17 [Content Brief]

[3]. Ferrajoli A, et al. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res, 2007, 67(23), 11291-11299. [Content Brief]

Cell Assay ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	To ascertain the inhibition of the immune populations within the spleen and peripheral blood compartments, tumor-bearing mice are treated with CTX, WP1066, or CTX in combination with WP1066, for 14 days. Single-cell suspensions are prepared from spleens and the peripheral blood of mice and single cells are surface-stained with FITC-conjugated anti-CD4 (L3T4) or PE-conjugated anti-CD8 (53-6.7) and are intracellularly stained with APC-conjugated-FoxP3 (clone FJK-16s). The cell number of CD4⁺ and CD8⁺ T cells in the peripheral blood is counted based on positive surface staining of the respective markers relative to the total cell count of PBMCs. The percentage of FoxP3+ Tregs is calculated within the peripheral blood and within the CD4 compartment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Verstovsek S, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res, 2008, (3), 788-796. [Content Brief] [2]. Hatiboglu MA, et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of WP1066 in murine melanoma models. Int J Cancer, 2012, 131(1), 8-17 [Content Brief] [3]. Ferrajoli A, et al. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res, 2007, 67(23), 11291-11299. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	2.8073 mL	14.0363 mL	28.0725 mL	70.1813 mL
	5 mM	0.5615 mL	2.8073 mL	5.6145 mL	14.0363 mL
	10 mM	0.2807 mL	1.4036 mL	2.8073 mL	7.0181 mL
	15 mM	0.1872 mL	0.9358 mL	1.8715 mL	4.6788 mL
	20 mM	0.1404 mL	0.7018 mL	1.4036 mL	3.5091 mL
	25 mM	0.1123 mL	0.5615 mL	1.1229 mL	2.8073 mL
	30 mM	0.0936 mL	0.4679 mL	0.9358 mL	2.3394 mL
	40 mM	0.0702 mL	0.3509 mL	0.7018 mL	1.7545 mL
DMSO	50 mM	0.0561 mL	0.2807 mL	0.5615 mL	1.4036 mL
	60 mM	0.0468 mL	0.2339 mL	0.4679 mL	1.1697 mL
	80 mM	0.0351 mL	0.1755 mL	0.3509 mL	0.8773 mL
	100 mM	0.0281 mL	0.1404 mL	0.2807 mL	0.7018 mL

WP1066 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WP1066857064-38-1WP 1066WP-1066STATJAKApoptosisJanus kinaseInhibitorinhibitorinhibit

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WP1066

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WP1066 Related Antibodies

25 Publications Citing Use of MCE WP1066

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All STAT Isoform Specific Products:

View All JAK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

WP1066 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

WP1066 Related Classifications

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