HPK1-IN-71
HPK1-IN-71 is a potent and selective HPK1 inhibitor with an IC50 of 26.3 nM. HPK1-IN-71 can inhibit the phosphorylation of SLP76, promote the secretion of IL-2 and show high selectivity for other kinases and immune-targeting kinases. HPK1-IN-71 can be used in colon cancer research.
For research use only. We do not sell to patients.
- Formula: C26H25FN8O
- Molecular Weight:484.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MAP4K Isoforms
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Biological Activity
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HPK1 63.00 μM (IC50) |
IL-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
63.00 μM
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Did not affect cell viability
Did not affect cell viability
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42335717 |
HPK1-IN-71 (compound D5) (0.11-1 μM; pretreatment for 30min + co-incubation with CD3/CD28 for 24h) leads to a modest yet statistically significant enhancement of IL-2 secretion at 0.33 μM, whereas the IL-2 stimulatory effect is diminished at 1 μM in primary mouse T cells[1].
HPK1-IN-71 (0-10 μM pretreatment for 2h + co-incubation with anti-CD3/CD28 antibodies for 10 min) leads to aconcentration-dependent reduction in SLP76 phosphorylation in Jurkat cells with significant inhibition at 1 μM and 10 μM[1].
HPK1-IN-71 (0-100 μM; 72 h) displays low cytotoxicity in Jurkat cells IC50= 63.00 μM)[1].
HPK1-IN-71 (1 μM; pretreatment for 60min + co-incubation with ADP-Glo™ reagent for 40min) only inhibits CDK2 and MST1 with > 80% inhibition, while exhibiting 50%-80% inhibition against just six other kinases. HPK1-IN-71 demonstrates high selectivity over LCK, IKKα and TAK1, all of which are directly involved in TCR signaling. HPK1-IN-71 displays moderate inhibition of GCK (MAP4K2), KHS (MAP4K5) and GLK (MAP4K3) with all inhibition rates below 80%. HPK1-IN-71 demonstrates a high degree of selectivity towards HGK (MAP4K4), MINK (MAP4K6) and all tested immune-related tyrosine kinases [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary mouse T cells
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Concentration:0.11 μM, 0.33 μM, 1 μM
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Incubation Time:pretreatment for 30min + co-incubation with CD3/CD28 for 24h
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Result:Promoted IL-2 secretion from primary mouse T cells at a concentration of 0.33 μM.
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Cell Line:Jurkat cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10μM
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Incubation Time:pretreatment for 2h + co-incubation with anti-CD3/CD28 antibodies for 10 min
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Result:Significantly downregulated SLP76 phosphorylation levels in Jurkat cells.
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Cell Line:Jurkat cells
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Concentration:3.13 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
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Incubation Time:72 h
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Result:Did not affect cell viability in Jurkat cells.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-inf | MRT |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 2.8 h | 0.2 h | 3289.0 ng/mL | 3739.0 ng·h/mL | 3867.3 ng·h/mL | 2.8 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (4-6 weeks old) were inoculated subcutaneously with CT26 cells (4 × 105 cells per mouse)[1].
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Dosage:10 or20 mg/kg
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Administration:i.p.; twice daily; for 13 days
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Result:Showedminimal antitumor efficacy at the dose of 10 mg/kg.
Showed significant antitumor potency with TGI of 37.2% at the dose of 20 mg/kg.
Did not change the mouse body weight.
Chemical Information
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Molecular Weight 484.53
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Formula C26H25FN8O
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SMILES
COC1=C(C2=CC3=C(NN=C3NC4=C5C=CC=CC5=NC(N6CCC(N)CC6)=N4)C=N2)C(F)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)