Famlasertib is a potent, brain-penetrant MAP4K inhibitor with IC50s value of 0.3 nM, 23.7 nM, and 44.7 nM for HGK (MAP4K4), MLK3, and MLK1, respectively. Famlasertib shows motor neuron protection and anti-inflammatory properties. Famlasertib can be used for the study of amyotrophic lateral sclerosis (ALS).

AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound.

BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.

PF 06260933 is a potent and selective MAP4K4 inhibitor (IC50 value 3.7 nM for MAP4K4 a.k.a. HGK or ZC1) with suitable PK properties in mouse to be used as a tool in an in vivo model of diabetes, vascular inflammation and atherosclerosis.

F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM.

HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.

BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers.

HPK1 inhibitor 1 is a highly potent, selective inhibitor of HPK1/MAP4K1 with biochemical IC50 of 0.0465 nM; displays >100-fold selectivity against 260 kinases in a panel of 265 kinases; HPK1 inhibitor 1 decreased SLP-76 phosphorylation in a human pSLP-76 ELISA at an IC50 lower than 0.02 uM; HPK1 inhibitor 1 enhanced Th1 cytokine production in T cells and fully reverted immune suppression imposed by the prostaglandin E2 (PGE2) and adenosine pathways in human T cells; HPK1 inhibitor 1 demonstrated a synergistic effect, resulting in enhanced interferon (IFN)-γ production when combination with pembrolizumab in human PBMCs

A-745 (A745) is a selective and potent HPK1 chemical probe (inhibitor) of HPK1.A-745 demonstrates an excellent cellular selectivity binding profile within pharmacologically relevant concentrations in unbiased cellular kinase-binding assays.A-745 exhibited in vitro immune cell activation phenotype reminiscent of Hpk1-deficient and Hpk1-kinase-dead T cells, including augmented proliferation and cytokine production.A-745 is a selective and potent small molecule HPK1 inhibitors with the pharmacological properties for immunotherapy.

HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM), HPK1-IN-21 also has orally active.

HPK1-IN-10 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-10 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 103) .

HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) .

HPK1-IN-16 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-16 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019051199A1, compound 39).

HPK1-IN-11 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-11 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 2).

HPK1-IN-17 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-17 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 73).

HPK1-IN-12 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-12 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 85) .

HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) .

HPK1-IN-18 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-18 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 1).

HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-14 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 79) .

HPK1-IN-15 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-15 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2018049200A1, compound 50).

GNE-495 is a potent and Selective MAP4K4 Inhibitor with IC50 of 3.7 nM.

HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.