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Signal Pathway Inhibitor


Product Name: Format/Size Descriptions Download
Signal Pathway Inhibitor Library 4817 compounds
For cherry-picking
Update: 2020-07
The file contains all available Signal Pathway Inhibitors selected from our Signature & BioDesign Libraries.
SL#003
Wnt/β-catenin Pathway Inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has screened 21000 small molecules in a luciferase reporter assay using the colorectal cancer cell lines, SW620 (APC mutation) and HCT116 (GSK3b mutation). Selected primary hits were optimized to yield an array of active compounds showing EC50 0.1-5 uM. The most promising compounds down regulate the expression of the key WNT oncogenes: DKK, cycD, CD44.
SL#012
Wnt/β-catenin Pathway Activators
80 compounds
Pre-Plated Set
Release: 2016
ASINEX, has screened a proprietary collection of 20000+ natural product like molecules, nucleoside mimetics, and glycomimetics in a luciferase reporter assay designed to monitor activation of the Wnt / β-catenin signaling pathway in C2C12 model cells. Primary hits were further optimized to generate a library of potent small molecule Wnt pathway activators with an EC50 range of 0.5-30 µM.
SL#024
STAT3 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has screened 10000+ natural product-like compounds in HepG2 cells transfected with the STAT3 reporter. As a result, several hit clusters were identified with sub uM potency in a cell-based assay. Structurally, the hit compounds incorporate several interesting natural product-like features such us bicyclic spiro-cores, iminosugars, and saturated fused rings. These compounds can be used as probes for further chemical biology studies across the STAT3 pathway.
SL#048
ApoE activators (agonist)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has screened a library of 15000 natural product like compounds in CCF-STTG (human astrocytoma) cells against ApoE secretion. A number of primary hits have been further optimized to provide compounds with ApoE secretion agonistic activity in the range of 0.6-15 µM.
SL#049
SMO inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has designed a library of small molecules sharing high structural similarity with approved drugs making them an interesting starting point for SMO-oriented drug discovery and research.
SL#075
WNT pathway inhibitors (PORCN)
80 compounds
Pre-Plated Set
Release: 2017
Analogs of GNF-1331 have been included in this library.

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Phenotypic Screening Sets: Format/Size Descriptions Download
Phenotypic Pre-Plated Set 13159 compounds
Pre-Plated Set
Amount: 0.01-2.0 mg
Update: 2020-07
ASINEX has created a diverse set of molecules by applying strict physico-chemical and structural descriptors to ensure good solubility and permeability properties.
Asinex in GOSTAR 1878 compounds
41742 analogues
For cherry-picking
Update: 2020-11
Asinex have opted to use the Global Online Structure Activity Relationship Database (GOSTAR) as an integrated source of data capturing chemical, biological, pharmacological, and therapeutic parameters. The structural overlap between the Asinex (500K+) and GOSTAR (8M+) databases has revealed 17910 unique molecules with associated biological activity. Application of additional structural filters (PAINS, Eli Lilly [4-5]) has resulted in a set of 11923 compounds; diversity-oriented selection supported by computational and medicinal chemistry expertise has further refined this set resulting in 1878 molecules available for computational or in vitro evaluation. Biological diversity is represented by multiple target families where each molecule is associated with a GOSTAR record via a unique structure code identifier.
SL#004
Oncology Phenotypic Screening-1
(Non-Macrocycle)
80 compounds / set
Pre-Plated Set
Update: 2016
ASINEX's oncology-oriented phenotypic library includes compounds based on several scaffolds with proven cytotoxicity (sub-µM EC50 in MTT assay) against a number of cancer cell lines: MV-411 (acute monocytic leukemia), HCT-116 (human colon cancer), MCF-7 (human breast adenocarcinoma‎), A-172 (Human glioblastoma), COLO-320 (colorectal adenocarcinoma), U-937 (histiocytic lymphoma), A-375 (malignant melanoma), BXPC-3 (pancreas adenocarcinoma), U118-MG (malignant glioma), and LN-229 (glioblastoma). Some active compounds were screened in a biochemical assay showing nM level of IC50 against several kinases: Aurora A, Haspin, VEGFR, EGFR, PDGFR.
SL#023
Oncology Phenotypic Screening-2
(Colon Cancer/Non-Macrocycle)
80 compounds / set
Pre-Plated Set
Update: 2016
ASINEX has evaluated the susceptibility of several colon cancer cell lines (HCT-116, SW-620, COLO-320, RKO) to a diverse array of small molecules and identified a series of related compounds that kill cancer cells at sub-µM concentrations with limited off target effect on healthy cells (human fibroblasts). Additional screening in a cell-based luciferase reporter assay of Wnt signaling has provided preliminary evidence of Wnt-dependent mechanism of action.
SL#035
Oncology Phenotypic Screening-3
(Macrocycles)
80 compounds / set
Pre-Plated Set
Update: 2016
ASINEX has evaluated the susceptibility of several cancer cell lines (i.e. RKO, HCT116, Molt-4, Rs4-11, U937, A549, H1568, H23, PANC1, A2780) to an array of peptidic and non-peptidic macrocycles and identified a series of compounds that kill cancer cells at µM concentrations.
Contact
Global

Ludmila Sadovenko

lsadovenko@asinex.com
North America

Mark Parisi

mparisi@asinex.com

Toll Free: +1 877 ASINEX1

Tel: +1 336 721 1617

Fax: +1 336 721 1618

N.Chestnut St., Ste.104

Winston-Salem, NC 27101

USA

Europe

Galina Afanasyeva

gafanasyeva@asinex.com

Tel: +31 (0) 203416183

Klaprozenweg 75C, 1033NN

Amsterdam, The Netherlands

Japan

Shingo Ota

sota@asinex.com

Tel: 080-3401-9097

30-2 Higashihazu, Nishio,

Aichi Japan

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