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WP1066

Specifications & Purity: ≥98%

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

Item Number
W129459
Grouped product items
SKU Size Availability Price Qty
W129459-10mg
10mg
Available within 1-2 weeks(?)
Item is derived from our semi-finished stock and is processed in 1-2 weeks.
$103.90
W129459-50mg
50mg
Available within 1-2 weeks(?)
Item is derived from our semi-finished stock and is processed in 1-2 weeks.
$462.90
W129459-250mg
250mg
Available within 1-2 weeks(?)
Item is derived from our semi-finished stock and is processed in 1-2 weeks.
$2,078.90
W129459-1g
1g
Available within 1-2 weeks(?)
Item is derived from our semi-finished stock and is processed in 1-2 weeks.
$7,480.90
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JAK/STAT3 inhibitor; AG 490 analog
main product photo

Basic Description

Synonyms (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide;(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide;WP-1066;WP 1066;STAT3 Inhibitor III
Specifications & Purity ≥98%
Storage Temp Store at 2-8°C
Shipped In Wet ice
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.
A cell permeable inhibitor of Stat3 and JAK2 protein tyrosine kinase.

Names and Identifiers

IUPAC Name (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
INCHI 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
Canonical SMILES CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N
PubChem CID 11210478
Molecular Weight 356.22

Certificates

Certificate of Analysis(COA)

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8 results found

Lot Number Certificate Type Date Item
J2130565 Certificate of Analysis Aug 02, 2023 W129459
J2130566 Certificate of Analysis Aug 02, 2023 W129459
E23121276 Certificate of Analysis Nov 08, 2022 W129459
E23121288 Certificate of Analysis Nov 08, 2022 W129459
E23121298 Certificate of Analysis Nov 08, 2022 W129459
E23121300 Certificate of Analysis Nov 08, 2022 W129459
E23121302 Certificate of Analysis Nov 08, 2022 W129459
E23121304 Certificate of Analysis Nov 08, 2022 W129459

Chemical and Physical Properties

Solubility DMSO 72 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements H302
Precautionary Statements P501,P264,P270,P330,P301+P317

Related Document

 SDS

 Specification Sheet

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Reviews

Customer Reviews

Associated Targets

CTH Tchem Cystathionine gamma-lyase 7 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

C7orf77 Tdark Uncharacterized protein C7orf77 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

C8orf34 Tbio Uncharacterized protein C8orf34 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CGGBP1 Tbio CGG triplet repeat-binding protein 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

C8orf76 Tdark Uncharacterized protein C8orf76 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CHD1 Tbio Chromodomain-helicase-DNA-binding protein 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CHERP Tbio Calcium homeostasis endoplasmic reticulum protein 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CHP1 Tbio Calcineurin B homologous protein 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CAMTA2 Tbio Calmodulin-binding transcription activator 2 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CNBD1 Tdark Cyclic nucleotide-binding domain-containing protein 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CNBD2 Tdark Cyclic nucleotide-binding domain-containing protein 2 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

COMTD1 Tdark Catechol O-methyltransferase domain-containing protein 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

NCAPD3 Tbio Condensin-2 complex subunit D3 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CMTR2 Tbio Cap-specific mRNA (nucleoside-2'-O-)-methyltransferase 2 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CTNNBIP1 Tbio Beta-catenin-interacting protein 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CNDP2 Tbio Cytosolic non-specific dipeptidase 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

PDE6H Tclin Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CTDNEP1 Tbio CTD nuclear envelope phosphatase 1 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CNFN Tdark Cornifelin 0 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

CNKSR1 Tchem Connector enhancer of kinase suppressor of ras 1 30 Activities

Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

References

1. Ferrajoli A, Faderl S, Van Q, Koch P, Harris D, Liu Z, Hazan-Halevy I, Wang Y, Kantarjian HM, Priebe W et al..  (2007)  WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells..  Cancer Res,  67  (23):  (11291-9).  [PMID:18056455]
2. Verstovsek S, Manshouri T, Quintás-Cardama A, Harris D, Cortes J, Giles FJ, Kantarjian H, Priebe W, Estrov Z.  (2008)  WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation..  Clin Cancer Res,  14  (3):  (788-96).  [PMID:18245540]
3. Bill MA, Fuchs JR, Li C, Yui J, Bakan C, Benson Jr DM, Schwartz EB, Abdelhamid D, Lin J, Hoyt DG et al..  (2010)  The small molecule curcumin analog FLLL32 induces apoptosis in melanoma cells via STAT3 inhibition and retains the cellular response to cytokines with anti-tumor activity..  Mol Cancer,  9  (11):  (165).  [PMID:20576164]
4. Tsujita Y, Horiguchi A, Tasaki S, Isono M, Asano T, Ito K, Asano T, Mayumi Y, Kushibiki T.  (2017)  STAT3 inhibition by WP1066 suppresses the growth and invasiveness of bladder cancer cells..  Oncol Rep,  38  (4):  (2197-2204).  [PMID:28849140]
5. Li M, Yu H.  (2021)  Identification of WP1066, an inhibitor of JAK2 and STAT3, as a KV 1.3 potassium channel blocker..  Br J Pharmacol,  178  (13):  (2617-2631).  [PMID:33689167]
6. Allaf A, Victoria B, Rosario R, Misztal C, Humayun Gultekin S, Dinh CT, Fernandez-Valle C.  (2022)  WP1066 induces cell death in a schwannomatosis patient-derived schwannoma cell line..  Cold Spring Harb Mol Case Stud,  8  (4):  (1531-6).  [PMID:35732500]
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