2. Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling
  3. Transmembrane Glycoprotein STAT
  4. 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.

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

TPST2-IN-1

TPST2-IN-1 Chemical Structure

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TPST2-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

STAT1

 

In Vitro

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.

TPST2-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MC38 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Increased phosphorylation of Stat1.
Parmacokinetics
Species Dose Route Note Clmax AUC
Mice 10 mg/kg p.o. 文献审核 374 ng/mL 1050 ng·h/mL
In Vivo

TPST2-IN-1 (Compound 77c) (50 mg/kg; intraperitoneal; daily; 1 day) inhibits tumor growth and enhances T-cell infiltration in subcutaneous MC38 colon carcinoma model in C57BL/6 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice with subcutaneous implantation of MC38 colon carcinoma cells (male, 6-8 weeks old, 18-20 g)[1]
Dosage: 50 mg/kg
Administration: Intraperitoneally injection;once a day
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
Molecular Weight

612.69

Formula

C31H34F2N4O5S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TPST2-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TPST2-IN-1Transmembrane GlycoproteinSTATimmunosuppression CD8 T cells interferon γ (IFNγ) receptor MC38 antitumor immunity tumor microenvironment anti-PD-1Inhibitorinhibitorinhibit

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HY-179288
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