TPST2-IN-1
TPST2-IN-1 is a potent and selective TPST2 inhibitor with an IC50 of 946 nM and a Ka of 19.4 μM. TPST2-IN-1 increases the phosphorylation of Stat1 and upregulates the IFNγ-responsive gene CXCL10 by inhibiting TPST2 activity.TPST2-IN-1 exhibits anti-tumor activity and enhances T cell-mediated antitumor immunity characterized by increased infiltration of effector CD8+ T cells. TPST2-IN-1 can be used for the research of cancer, such as colon cancer.
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- 화학식: C31H34F2N4O5S
- 분자량:612.69
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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STAT1 |
TPST2-IN-1 (Compound 77c) (0.5-1 μM, 24-48 h) enhances IFNγ-induced Cxcl10 gene expression, promotes Stat1 phosphorylation in MC38 cells, and reduces the tyrosine sulfation level of interferon γ receptor 1 (IFNGR1) in HEK293 cells[1].
TPST2-IN-1 (2 μM, 1 h) enhances the thermal stability of TPST2 in MDA-MB-231 cells overexpressing Flag-TPST2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MC38 cells
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Increased phosphorylation of Stat1.
| Species | Dose | Route | Note | Clmax | AUC |
|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 文献审核 | 374 ng/mL | 1050 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice with subcutaneous implantation of MC38 colon carcinoma cells (male, 6-8 weeks old, 18-20 g)[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneally injection;once a day
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Result:Inhibited tumor growth.
\r\nIncreased the infiltration of effector CD8+ T cells, memory CD8+ T cells and NK cells in the spleen and tumor tissues.
\r\nEnhanced systemic immune activation.
\r\n
Chemical Information
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분자량 612.69
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화학식 C31H34F2N4O5S
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SMILES
O=C(C[C@@H]1CC[C@H](CC1)C2=CC=C(C=C2)N3CCN(CC3)C(CCC(NC4=NC(C5=CC(F)=C(C(F)=C5)O)=CS4)=O)=O)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TPST2-IN-1 Related Classifications
HY-179288 Related Classifications
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