2. MAPK/ERK Pathway Cell Cycle/DNA Damage Immunology/Inflammation
  3. MAP4K HOXA Interleukin Related
  4. HPK1-IN-65

HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research.

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HPK1-IN-65

HPK1-IN-65 Chemical Structure

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HPK1-IN-65 Related Antibodies

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Description

HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research[1].

IC50 & Target[1]

HPK1

<5 nM (IC50)

IL-2

398 nM (EC50)

In Vitro

HPK1-IN-65 (compound 34) decreases pSLP76 in a dose-dependent manner in Jurkat cell line with IC50 values of 92.3 nM[1].
HPK1-IN-65 stimulates IL- 2 production with an EC50 of 398 nM and enhances the activation up to 3.59 fold[1].
HPK1-IN-65 has the anti proliferative effect in Jurkat cells[1].
HPK1-IN-65 has selectivity against MAP4K2, MAP4K3, MAP4K4, MAP4K5, MAP4K6[1].

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

HPK1-IN-65 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 AUC CL Vdss Cmax F
Rat[1] 1 mg/mL i.v. 2.9 h 1786.7 ng·h/mL 9.7 mL/min/kg 1.6 L/kg / /
Rat[1] 10 mg/kg p.o. 2.8 h 1217.0 ng·h/mL / / 2633.3 ng/mL 66.7 %
In Vivo

HPK1-IN-65 (compound 34) (60 mg/kg, p.o., once daily for 14 consecutive days) exhibits a robust anti tumor response in the CT 26 syngeneic tumor model in female BALB/c mice (6 weeks old)[1].

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

Animal Model: Colorectal carcinoma cell line CT-26 cells (2.5 × 105 cells, s.c.) induced female BALB/c mice (6- week-old)[1]
Dosage: 60 mg/kg
Administration: i.g., once daily for 14 consecutive days, Anti-PD-1 monoclonal antibody (HY-P99709) (i.p., 10 mg/kg, twice a week)
Result: Achieved a robust anti-tumor response with a TGI of 62.90%.
Caused no significant impact on animal body weight in either monotherapy or combination groups.
Delayed the tumor growth, with the tumor growth inhibi tion (TGI) reaching 41.73 % at 14 days post-treatment (without Anti-PD-1 monoclonal antibody).
Molecular Weight

528.99

Formula

C23H22ClFN8O2S
SMILES

FC1=C(NC2=NC=C(Cl)C(NC3=C(NS(C)(=O)=O)C(N=CC=N4)=C4C=C3)=N2)C=C5C(CCN(C)C5)=C1
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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HPK1-IN-65 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:

HPK1-IN-65MAP4KHOXAInterleukin RelatedMAPK Kinase Kinase KinaseHomeobox AILHPK1 inhibitorMAP4K kinasetumor efficacySer376Inhibitorinhibitorinhibit

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