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TPST2-IN-1 is a potent and selective TPST2 inhibitor, with an IC50 of 946 nM and a Ka of 19.4 μM. It functions by inhibiting TPST2 activity, thereby increasing the phosphorylation level of Stat1 and upregulating the expression of the IFNγ-responsive gene CXCL10. Exhibiting antitumor activity, TPST2-IN-1 enhances T cell-mediated antitumor immunity, characterized by increased infiltration of effector CD8+ T cells. This compound is applicable in cancer research, such as studies involving colorectal cancer.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | TPST2-IN-1 is a potent and selective TPST2 inhibitor, with an IC50 of 946 nM and a Ka of 19.4 μM. It functions by inhibiting TPST2 activity, thereby increasing the phosphorylation level of Stat1 and upregulating the expression of the IFNγ-responsive gene CXCL10. Exhibiting antitumor activity, TPST2-IN-1 enhances T cell-mediated antitumor immunity, characterized by increased infiltration of effector CD8+ T cells. This compound is applicable in cancer research, such as studies involving colorectal cancer. |
| In vitro | TPST2-IN-1 (Compound 77c) enhances IFNγ-induced Cxcl10 gene expression in MC38 cells and promotes STAT1 phosphorylation at concentrations of 0.5-1 μM over 24-48 hours, while it reduces the tyrosine sulfation level of IFNγ receptor 1 (IFNGR1) in HEK293 cells. Additionally, TPST2-IN-1 at 2 μM for 1 hour increases the thermal stability of TPST2 in MDA-MB-231 cells that overexpress Flag-TPST2. |
| In vivo | TPST2-IN-1 (Compound 77c) (50 mg/kg; intraperitoneal injection; daily; 1 day) inhibits tumor growth and enhances T cell infiltration in a subcutaneous MC38 colon cancer model in C57BL/6 mice. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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