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SML1585

Sigma-Aldrich

ML116

≥95% (HPLC)

Synonym(s):

4-Benzyl-1-{thieno[2,3-d]pyrimidin-4-yl}piperidine, 4-[4-(Phenylmethyl)-1-piperidinyl]-thieno[2,3-d]pyrimidine, CID 2100018

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About This Item

Empirical Formula (Hill Notation):
C18H19N3S
CAS Number:
Molecular Weight:
309.43
UNSPSC Code:
12352202
NACRES:
NA.77

assay

≥95% (HPLC)

form

powder

color

white to brown

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

room temp

InChI

1S/C18H19N3S/c1-2-4-14(5-3-1)12-15-6-9-21(10-7-15)17-16-8-11-22-18(16)20-13-19-17/h1-5,8,11,13,15H,6-7,9-10,12H2

InChI key

AJQCKNBBHOVJGO-UHFFFAOYSA-N

General description

The gene STAT3 (signal transducer and activator of transcription 3) is mapped to human chromosome 17q21.[1] The protein contains a SH2 (src homology 2) domain.[2]

Biochem/physiol Actions

ML116 is a potent and selective inhibitor of STAT3 (signal transducer and activator of transcription 3) phosphorylation. ML116 potently inhibits growth and induces cell death of rodent and human glioma cells. ML116 is inactive against the related STAT1 and NFkB anti-targets.
ML116 is a potent and selective inhibitor of STAT3.
STAT3 is a transcription factor which is activated by cytokines and growth factors. It is oncogenic and is present in various cancers, such as breast, prostate, renal cell, melanoma, ovarian, lung, leukemia, lymphoma and myelomas.[2] It is associated with cellular growth, survival and malignancy.[3]

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Hikmat H Assi et al.
The Journal of pharmacology and experimental therapeutics, 349(3), 458-469 (2014-04-04)
Signal transducer and activator of transcription 3 (STAT3) has been implicated as a hub for multiple oncogenic pathways. The constitutive activation of STAT3 is present in several cancers, including gliomas (GBMs), and is associated with poor therapeutic responses. Phosphorylation of
Aijaz Parray et al.
Biologics : targets & therapy, 6, 267-276 (2012-09-08)
The treatment landscape for patients with castration-resistant prostate cancer (CRPC) is undergoing significant changes with the advent of new therapies and multidisciplinary efforts by scientists and clinicians. As activation of multiple molecular pathways in the neoplastic prostate makes it impossible
Y T Tsai et al.
Molecular and cellular biology, 20(6), 2043-2054 (2000-02-25)
Etk (also called Bmx) is a member of the Btk tyrosine kinase family and is expressed in a variety of hematopoietic, epithelial, and endothelial cells. We have explored biological functions, regulators, and effectors of Etk. Coexpression of v-Src and Etk
E Y M G Fung et al.
Genes and immunity, 10(2), 188-191 (2008-12-27)
As a result of genome-wide association studies in larger sample sets, there has been an increase in identifying genes that influence susceptibility to individual immune-mediated diseases, as well as evidence that some genes are associated with more than one disease.
Huang Shao et al.
Cancer research, 63(14), 3923-3930 (2003-07-23)
The oncogene signal transducer and activator of transcription 3 (Stat3) is constitutively activated in a wide variety of human cancers, including squamous cell carcinoma of the head and neck. In squamous cell carcinoma of the head and neck, Stat3 activation

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