1. Immunology/Inflammation
  2. LILRB
  3. ES009

ES009 is a high-affinity LILRB2 antagonist, with IC50 values of 14.07 nM and 18.61 nM for inhibiting hLILRB2-huANGPTL3 and hLILRB2-huANGPTL4, respectively. ES009 specifically blocks the interactions between LILRB2 and MHC class I as well as non-MHC ligands, thereby effectively inhibiting receptor activation. ES009 can reprogram anti-inflammatory myeloid cells and induce their conversion to a pro-inflammatory phenotype, and also reverse the T cell suppression mediated by macrophages. When combined with anti-PD-1 blockade therapy, ES009 synergistically enhances T cell activation. ES009 can be used in research related to advanced solid tumors and ovarian cancer.

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ES009

ES009 Chemical Structure

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Description

ES009 is a high-affinity LILRB2 antagonist, with IC50 values of 14.07 nM and 18.61 nM for inhibiting hLILRB2-huANGPTL3 and hLILRB2-huANGPTL4, respectively. ES009 specifically blocks the interactions between LILRB2 and MHC class I as well as non-MHC ligands, thereby effectively inhibiting receptor activation. ES009 can reprogram anti-inflammatory myeloid cells and induce their conversion to a pro-inflammatory phenotype, and also reverse the T cell suppression mediated by macrophages. When combined with anti-PD-1 blockade therapy, ES009 synergistically enhances T cell activation. ES009 can be used in research related to advanced solid tumors and ovarian cancer[1][2][3].

Isotype

Human IgG4 kappa

Recommend Isotype Controls
Species Reactivity

Human

IC50 & Target[1]

LILRB2

 

In Vitro

ES009 binds to human LILRB2 overexpressed on EL4-huLILRB2 cells, with an EC50 of 0.49 nM[1].
ES009 potently blocks the interactions between human LILRB2 and the MHC class I ligands HLA-G and HLA-A2 on EL4-huLILRB2 cells, with IC50 values of 0.16 nM and 0.24 nM, respectively[1].
ES009 induces a proinflammatory phenotype in human monocyte-derived dendritic cells by blocking LILRB2[3].

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

In Vivo

ES009 (15-206 mg/kg; i.v.; single dose) exhibits an excellent safety profile in SD rats, with no detectable off-target toxic effects at doses up to 206 mg/kg and no impact on central nervous system or respiratory function at doses up to 135 mg/kg[1].

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

Animal Model: Sprague-Dawley (SD) (male and female)[1]
Dosage: 15 mg/kg; 45 mg/kg; 100 mg/kg; 135 mg/kg; 206 mg/kg
Administration: i.v.; single dose
Result: Showed no ES009-related adverse effects across all tested doses, including no changes in clinical signs, body weight, food consumption, clinical pathology, immunotoxicity, or histopathology.
Detected no effects on central nervous system function or respiratory system function up to 336 hours post-dose.
Determined the maximum tolerated dose to be 206 mg/kg, the highest feasible dose tested.
Gene ID

10288  [NCBI]

Accession
Target

LILRB2/ILT4

Application

ELISA, FACS, Functional assay

Conjugated

Unconjugated

Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.

Formulation

Please refer to the lot-specific COA for specific buffer information.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
ES009
Cat. No.:
HY-P992353
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