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Cat. No.: HY-P991179

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Biologically Validated

MK-4166

Name: MK-4166
Brand: MedChemExpress
SKU: HY-P991179
Price: 280.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Based on 1 Customer Validation

MK-4166 is a humanized IgG1 agonist anti-human GITR monoclonal antibody. MK-4166 triggers the downstream NF-κB signaling pathway through activation of GITR, and downregulates FOXP3 expression in tumor-infiltrating Tregs, thereby attenuating the immunosuppressive microenvironment and promoting T cell activation. MK-4166 can be used for research on various solid tumors.

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Pureté : 98.20%
Masse moléculaire:145.2 kDa

Stockage:

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

MK-4166 Chemical Structure

Size

Prix

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Quantité

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Isotype
- Recommend Isotype Controls
- Species Reactivity
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
- Gene ID
- Accession
- Conjugated
- Reconsititution
- Application
- Verified Bioactivity
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Isotype

Human IgG1 kappa

Recommend Isotype Controls

Human IgG1 kappa, Isotype Control

Species Reactivity

Human

IC₅₀ & Target

^[1]

GITR

Voir tous les produits spécifiques à Isoform TNF Receptor :

Voir tous les produits spécifiques à Isoform NF-κB :

In Vitro

Adaptive ImmunityAnti-cancerCytokines & ChemokinesImmune Tolerance & ImmunosuppressionOthers

Adaptive Immunity

MK-4166 (4-5 days) increases the proliferation of human and cynomolgus monkey naive CD4⁺ T cells stimulated with anti-human CD3 mAb (clone UCHT1) (HY-P991842), with median EC₅₀ values of 7.7 pM and 7.9 pM, respectively^[1].

Adaptive Immunity

Anti-cancer

MK-4166 (10 µg/mL; 7 days) increases the proliferation of anti-CD3 mAb (clone OKT3) (HY-P990864)-stimulated human NSCLC TILs^[1].

Adaptive Immunity

Anti-cancer

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

MK-4166 (10 μg/mL; 1-7 days) upregulates DUSP6 gene expression at 24 h and downregulates FOXP3 gene expression at 7 days in CD4+ TILs from single-cell suspensions of human RCC and CRC^[1].

Adaptive Immunity

Anti-cancer

Immune Tolerance & Immunosuppression

MK-4166 (5 μg/mL; 5-30 min) rapidly induces NF-κB p65 phosphorylation in MLR-derived Tregs and effector T cells and in human TILs^[1].

Adaptive Immunity

Immune Tolerance & Immunosuppression

MK-4166 (4-7 days) attenuates the suppression of effector CD4+ and CD8+ T cell proliferation by nTregs in co-cultured effector T cells and nTregs in the nTreg suppression assay^[1].

Adaptive Immunity

Immune Tolerance & Immunosuppression

Cytokines & Chemokines

MK-4166 (0.1-20 μg/mL; 7 days) dose-dependently reduces induced Tregs (iTregs) generation in mixed lymphocyte reaction (MLR) cultures^[1].

Others

MK-4166 binds human and cynomolgus monkey GITR with high affinity, with affinities of 5.5 pM and 7.6 pM, respectively, but does not bind mouse GITR^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

TILs
Concentration:

10 µg/mL
Incubation Time:

7 days
Result:

Increased the proliferation of human NSCLC TILs stimulated by anti-CD3 mAb (clone OKT3).

In Vivo

Anti-cancerAdaptive ImmunityImmune Tolerance & ImmunosuppressionCytokines & Chemokines

Anti-cancer

Adaptive Immunity

Immune Tolerance & Immunosuppression

Cytokines & Chemokines

MK-4166 (10 mg/kg; s.c.; single administration; 49 days) reduces peripheral Treg frequency, attenuates the intratumoral Treg suppressive phenotype (decreased ICOS expression), increases effector cytokine (IL2 and IFNγ) production, and significantly inhibits tumor growth in hu-CD34+ NSG humanized mice engrafted with human SK-MEL-5 melanoma cells^[3].

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

Animal Model:

NSG (hu-CD34+; NOD.Cg-PrkdcscidIl2rgtm1Wjl; reconstituted with human CD34+ hematopoietic stem cells; >25% human immune cell chimerism at 12 or more weeks post-reconstitution)^[4]
Dosage:

10 mg/kg
Administration:

s.c.; single dose; 4, 49 days
Result:

Significantly reduced the frequency of Tregs in the spleen and showed a trend toward reduced Treg frequency in the tumor.
Reduced the expression of the activation marker ICOS on intratumoral Tregs, indicating attenuated suppressive function.
Increased the production of antitumor effector cytokines (such as IL-2 and IFNγ) within the tumor.
Significantly attenuated tumor growth compared to the isotype control group.

Related Protocols :

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Gene ID

8784 [NCBI]

Accession

Q9Y5U5

Conjugated

Unconjugated

Reconsititution

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

Application

ELISA, FACS, Functional assay

Verified Bioactivity

Flow cytometric analysis of 1X10⁶ Jurkat cells with MK-4166 (HY-P991179, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa (HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Immobilized Human GITR/TNFRSF18 Protein, His Tag can bind MK-4166. The EC₅₀ for this effect is 85.95 ng/mL.

Chemical Information

Appearance Liquid
Masse moléculaire 145.2 kDa
Color Colorless to light yellow
SMILES

[MK-4166]
Livraison

Shipping with dry ice.
Formulation

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

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Inhibitory Antibodies User Guide (603 KB)

Références

[1]. Sukumar S, et al. Characterization of MK-4166, a Clinical Agonistic Antibody That Targets Human GITR and Inhibits the Generation and Suppressive Effects of T Regulatory Cells. Cancer research. 2017 Aug 15;77(16):4378-4388. [Content Brief]

[2]. Bhamra I, et al. Novel Porcupine inhibitor RXC004: Potent efficacy in animal models of cancer through direct tumour targeting and immunomodulatory mechanisms. European Journal of Cancer. 2016 Dec 1;69:S100-1.

[3]. Mahne AE, et al. Dual Roles for Regulatory T-cell Depletion and Costimulatory Signaling in Agonistic GITR Targeting for Tumor Immunotherapy. Cancer research. 2017 Mar 01;77(5):1108-1118.

[4]. Smith PL, et al. Directing T-cell immune responses for cancer vaccination and immunotherapy. Vaccines. 2021 Nov 25;9(12):1392.

[5]. Wang Y, et al. GITRL on dendritic cells aggravates house dust mite-induced airway inflammation and airway hyperresponsiveness by modulating CD4 T cell differentiation. Respiratory research. 2021 Feb 08;22(1):46. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Activité biologique
- Description
- Isotype
- Recommend Isotype Controls
- Species Reactivity
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
- Gene ID
- Accession
- Conjugated
- Reconsititution
- Application
- Biological Activity
Chemical Information
Pureté et documentation
Références

1/16

Flow cytometric analysis of 1X10⁶ Jurkat cells with MK-4166 (HY-P991179, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa (HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
1/16

Immobilized Human GITR/TNFRSF18 Protein, His Tag can bind MK-4166. The EC₅₀ for this effect is 85.95 ng/mL.
1/16

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MK-4166

Cytotoxicity LDH Assay Kit

PBS Buffer (1×)

DPBS Buffer (1×)

Voir tous les produits spécifiques à Isoform TNF Receptor

Voir tous les produits spécifiques à Isoform NF-κB

Activité biologique

Description

Isotype

Recommend Isotype Controls

Species Reactivity

IC50 & Target

In Vitro

In Vivo

Essai clinique

Gene ID

Accession

Conjugated

Reconsititution

Application

Verified Bioactivity

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MK-4166 Related Classifications

HY-P991179 Related Classifications

Bioz

Keywords

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