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Chemical Structure| 1507095-58-0 Chemical Structure| 1507095-58-0

Structure of TWS119 TFA
CAS No.: 1507095-58-0

Chemical Structure| 1507095-58-0

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TWS119 TFA is a specific GSK-3β inhibitor with an IC50 of 30 nM and activates the Wnt/β-catenin pathway.

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Product Details of TWS119 TFA

CAS No. :1507095-58-0
Formula : C22H16F6N4O6
M.W : 546.37
SMILES Code : NC1=CC(C2=CC3=C(OC4=CC(O)=CC=C4)N=CN=C3N2)=CC=C1.O=C(C(F)(F)F)O.O=C(C(F)(F)F)O
MDL No. :MFCD09037535
InChI Key :XJEFPMFFWJTJSL-UHFFFAOYSA-N
Pubchem ID :90488884

Safety of TWS119 TFA

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of TWS119 TFA

PI3K-AKT
Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human CD4+ T cells 5 µM 14 days Induction of T SCM cells EBioMedicine. 2016 Jan 16;4:50-61.
Human CD8+ T cells 5 µM 14 days Induction of T SCM cells EBioMedicine. 2016 Jan 16;4:50-61.
Mouse brain microvascular endothelial cell line bEnd.3 10 µM 12 hours TWS119 promoted angiogenesis in OGD bEnd.3 cells by modulating microglial polarization and ameliorating the inflammatory microenvironment J Neuroinflammation. 2019 Dec 6;16(1):256.
Primary mouse embryonic stem cells 1–5 µM 2 days To induce neuronal differentiation Proc Natl Acad Sci U S A. 2003 Jun 24;100(13):7632-7.
Rat cardiomyocytes 0.8 µM 24 hours To evaluate the effect of TWS119 on Wnt signaling, the results showed that TWS119 treatment enhanced Wnt signaling activity, leading to a significant decrease in Cdon protein levels and up-regulation of cell surface Cx43 proteins, resulting in increased Lucifer Yellow dye transfer. Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):E1345-E1354.
Primary microglia 10 µM 24 hours TWS119 promoted the switch of microglia from pro-inflammatory to anti-inflammatory phenotype, possibly mediated by the Wnt/β-catenin signaling pathway J Neuroinflammation. 2019 Dec 6;16(1):256.
T memory stem cells (Tscm) 5 mM 3 days To induce differentiation of naive T cells into Tscm cells and expand them. Front Immunol. 2024 Jul 5;15:1367609.
HT-29 cells 10 µM 4 hours To uncouple the nuclear and cytoplasmic functions of p38α and assess its role in the Wnt signaling pathway. Results showed that TWS-119 promoted nuclear translocation of β-catenin and p38α. Cell Biosci. 2023 Dec 1;13(1):223.
HCT-116 cells 10 µM 4 hours To uncouple the nuclear and cytoplasmic functions of p38α and assess its role in the Wnt signaling pathway. Results showed that TWS-119 promoted nuclear translocation of β-catenin and p38α. Cell Biosci. 2023 Dec 1;13(1):223.
Human peripheral blood lymphocytes 5 µM 7 days Enrichment of T SCM cells by differentiation inhibitor TWS119, resulting in a 100-fold increase in T SCM numbers Stem Cell Res Ther. 2018 Dec 7;9(1):337.
HMLE-Snail cells 2 µM To evaluate the effects of TWS119 on EMT and stem cell properties, results showed that TWS119 significantly reduced the expression of mesenchymal markers and inhibited cell migration. Breast Cancer Res. 2019 Mar 7;21(1):37.
HMLE-Twist cells 2 µM To evaluate the effects of TWS119 on EMT and stem cell properties, results showed that TWS119 significantly reduced the expression of mesenchymal markers and inhibited cell migration. Breast Cancer Res. 2019 Mar 7;21(1):37.
SUM159 cells 2 µM To evaluate the effects of TWS119 on EMT and stem cell properties, results showed that TWS119 significantly reduced the expression of mesenchymal markers and inhibited cell migration. Breast Cancer Res. 2019 Mar 7;21(1):37.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Ischemic stroke model induced by permanent distal middle cerebral artery occlusion plus 1 h hypoxia Intraperitoneal injection 10 mg/kg Once daily for 14 days TWS119 ameliorated the neuroinflammatory microenvironment following ischemic stroke by modulating microglia toward an anti-inflammatory phenotype and facilitated neurological recovery J Neuroinflammation. 2019 Dec 6;16(1):256.
Mice APCMin/+ mice Intraperitoneal injection 14 mg/kg Once a week for 5 weeks To evaluate the effect of the p38α inhibitor SB202190 on colon tumors in APCMin/+ mice. Results showed that SB202190 significantly reduced the number of colon tumors. Cell Biosci. 2023 Dec 1;13(1):223.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01087294 Leukemia, B-cell ... More >> Lymphoma, Hodgkins Lymphoma, Non-hodgkins Lymphoma, B-Cell Less << Phase 1 Recruiting March 1, 2024 United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office    (888) NCI-1937       Contact: Referral Line NCI Experimental Transplantation and Immunology Branch    (301) 435-5942    nci-transplant@mail.nih.gov Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.15mL

1.83mL

0.92mL

18.30mL

3.66mL

1.83mL

 

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