2. MAPK/ERK Pathway
  3. MAP4K
  4. HPK1-IN-62

HPK1-IN-62 is a selective and orally active HPK-1 inhibitor with an IC50 of 1.22 nM. HPK1-IN-62 significantly improves GLK selectivity (> 665-fold) and LCK selectivity (> 1095-fold). HPK1-IN-62 enhances T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1 therapy in the MC38 tumor model, inhibiting a tumor growth. HPK1-IN-62 can be used in the researchs of colon cancer and cancer immunotherapy.

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

HPK1-IN-62

HPK1-IN-62 Chemical Structure

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HPK1-IN-62 Related Antibodies

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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Description

HPK1-IN-62 is a selective and orally active HPK-1 inhibitor with an IC50 of 1.22 nM. HPK1-IN-62 significantly improves GLK selectivity (> 665-fold) and LCK selectivity (> 1095-fold). HPK1-IN-62 enhances T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1 therapy in the MC38 tumor model, inhibiting a tumor growth. HPK1-IN-62 can be used in the researchs of colon cancer and cancer immunotherapy[1].

IC50 & Target[1]

HPK1

1.22 nM (IC50)

GLK/MAP4K3

812 nM (IC50)

GCK/MAP4K2

1336.9 nM (IC50)

In Vitro

HPK1-IN-62 (Compound 2t) (0-10 μM ,5.2 h) is effective in inhibiting the phosphorylation of SLP76 in peripheral blood mononuclear cells (PBMCs) with an IC50 of 1.7 μM[1].
HPK1-IN-62 (1 μM) exhibits excellent metabolic stability in human liver microsomes[1].

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

HPK1-IN-62 Related Antibodies
In Vivo

HPK1-IN-62 (Compound 2t) (100 mg/kg, p.o., twice daily for 14 days) shows synergistic effects with anti-mPD-1 antibodies in the MC38 mouse model[1].

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

Animal Model: MC38 cells xenograft model established in female C57BL/6 mice, aged 6-7 weeks[1]
Dosage: 100 mg/kg with or without anti-mPD-1
Administration: Oral administration (p.o.), twice daily for 14 days
Result: Did not show significant tumor-suppressive effects as monotherapy.
Enhanced T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1, achieving a tumor growth inhibition (TGI) rate of 76%, compared to 70% with anti-mPD-1 monotherapy.
Molecular Weight

563.65

Formula

C32H33N7O3
SMILES

N#CC1=C2C=C(NC3=NC(N[C@@H](C4=C(OCCCC2)C=CC=C4)CO)=C(C=N3)C5=CC(N6CC[C@H](C6)O)=NC=C5)C=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-62 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-62MAP4KMAPK Kinase Kinase KinaseCancer immunotherapyHPK1 kinase inhibitorMacrocyclizationPyridineSelectivityInhibitorinhibitorinhibit

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