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HPK1-IN-65 is a selective, orally active HPK1 inhibitor with an IC50 value of less than 5 nM, demonstrating 1257-fold selectivity over the MAP4K kinase family member GLK. It inhibits pSLP76 phosphorylation with an IC50 of 92.3 nM and stimulates IL-2 production with an EC50 of 398 nM. Additionally, HPK1-IN-65 suppresses the phosphorylation of the TCR-induced SLP76Ser376 site in a dose-dependent manner. This compound is also applicable in colon cancer research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | HPK1-IN-65 is a selective, orally active HPK1 inhibitor with an IC50 value of less than 5 nM, demonstrating 1257-fold selectivity over the MAP4K kinase family member GLK. It inhibits pSLP76 phosphorylation with an IC50 of 92.3 nM and stimulates IL-2 production with an EC50 of 398 nM. Additionally, HPK1-IN-65 suppresses the phosphorylation of the TCR-induced SLP76Ser376 site in a dose-dependent manner. This compound is also applicable in colon cancer research. |
| Targets&IC50 | HPK1:<5 nM |
| In vitro | HPK1-IN-65 (compound 34) reduces pSLP76 levels in Jurkat cells in a dose-dependent manner, with an IC50 of 92.3 nM. It stimulates IL-2 production with an EC50 of 398 nM, enhancing the activation effect up to 3.59-fold. Additionally, HPK1-IN-65 exhibits antiproliferative effects on Jurkat cells and shows selectivity for MAP4K2, MAP4K3, MAP4K4, MAP4K5, and MAP4K6. |
| In vivo | HPK1-IN-65 (compound 34), administered orally at a dose of 60 mg/kg once daily for 14 consecutive days, demonstrates potent antitumor activity in a CT-26 syngeneic tumor model using female BALB/c mice aged six weeks. |
| 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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