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ZYF0033

ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376) . ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a+CD8+ T cells, but not T cells, PD-1+CD8+ T cells, TIM-3+CD8+ Infiltration of T cells and LAG3+CD8+ T cells was reduced[1][2].

Product Specifications

CAS Number

[2380300-79-6]

Product Name Alternative

HPK1-IN-22

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

MAP4K

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/zyf0033.html

Purity

98.86

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC(C)(C)C#CC1=CC=CC(COC2=C(N)N=CC(C3=CN=C(C4CCN(CC4)C)S3)=C2)=C1

Molecular Formula

C26H30N4O2S

Molecular Weight

462.61

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362-P403+P233-P405-P501

References & Citations

[1]Jingwen Si, et al. Hematopoietic Progenitor Kinase1 (HPK1) Mediates T Cell Dysfunction and Is a Druggable Target for T Cell-Based Immunotherapies. Cancer Cell. 2020 Oct 12;38 (4) :551-566.e11.|[2]Si J, et al. Hematopoietic Progenitor Kinase1 (HPK1) Mediates T Cell Dysfunction and Is a Druggable Target for T Cell-Based Immunotherapies. Cancer Cell. 2020 Oct 12;38 (4) :551-566.e11.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

MAP4K1/HPK1

Available Sizes

Curated Selection

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