YK012
YK012 is an anti-CD19 and CD3 T cell engager with a Kd of 1.96 μM for hCD3 ε/δ and a Kd of approximately 0.5 nM for hCD19. YK012 binds CD3/TCR and activates cells only upon crosslinking by CD19-positive target cells. YK012 induces cytokine release (IL-2, TNF-α, IFN-γ, IL-6) as well as granzyme B/perforin release. YK012 alleviates pathological symptoms in a collagen-induced arthritis model. YK012 exhibits extremely low antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) activity, and does not mediate killing of CD19-negative cells. YK012 can be used for research on rheumatoid arthritis.
For research use only. We do not sell to patients.
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Species Reactivity
Human
IC50 & Target
[1]|
IL-2 |
IL-6 |
In Vitro
YK012 binds recombinant hCD3 ε/δ with low intrinsic affinity (KD = 1.96 μM) in cell-free BIAcore assays and binds hCD19 with high affinity (approximately 0.5 nM)[1].
YK012 (30 min) binds membrane CD19 on Raji-lp cells with an apparent KD = 1.3 nM and binds B cells with an EC50 = 20.28 ng/mL, whereas membrane CD3 on Jurkat T cells has an apparent KD = 124 nM[1].
YK012 (1 µg/mL; 72 h) increased CD25+CD8+ T cells from 0.3% to 10.9% only when PBMC-derived T cells were co-cultured with CD19+ Raji cells[1].
YK012 (starting at 8 nM, 4-fold dilution; 2-24 hours) mediated time-dependent T cell cytotoxicity against CD19+ Raji-luc and NALM6-luc, with nearly complete killing at >10 pM after 24 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
YK012 (0.1-0.5 mg/kg; i.v. via tail vein injection; twice a week for a total of 7 doses; D0, D3, D7, D10, D14, D17, D21) depletes peripheral blood CD79b+ B cells in huHSC-NCG-M mice, with 0.1 mg/kg showing greater depletion than 0.5 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hCD3EDG/hCD19 transgenic on C57BL/6 background (male; 8 weeks old)[1]
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Dosage:0.125 mg/kg (Group C); 0.25 mg/kg (Group D); 0.5 mg/kg (Group E)
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Administration:Day 27 to Day 73; total 15 administrations; frequency adjusted
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Result:Joint scoring showed a downward trend in joint scores of YK012 dose groups compared with the model group.
Protein level detection did not reveal differences in CRP, RF, ACPA, and SAA levels among groups.
Joint pathological staining scores showed a downward trend.
Flow cytometry demonstrated changes (fluctuations) in absolute counts of peripheral blood B cells (CD20+/B220+) and T cells (TCRβ+) and their proportions, beginning on Day 33 (6 days after first administration) and partially or fully recovering in later stages of the experiment.
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Animal Model:HuHSC-NCG-M[1]
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Dosage:G1 0.1 mg/kg; G2 0.5 mg/kg
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Administration:i.v. via tail vein injection; twice a week for a total of 7 doses on D0, D3, D7, D10, D14, D17, D21
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Result:Before grouping, the average level of hCD45×hCD3 in mice was 3.31%.
After YK012 administration via tail vein injection twice a week for a total of 7 doses, there was a reduction in the number of B cells (CD79b+) in peripheral blood.
The B cell depletion effect of G1 (0.1 mg/kg) was superior to that of G2 (0.5 mg/kg).
All YK012 groups showed depletion of B cell (CD79b+) proportion and number on D1, D7, D11, D14, and D21 compared to D-5, with the degree of decrease deepening with time and number of doses.
Group G1: B cell proportion on D7 decreased; B cell proportion on D11, D14, and D21 decreased more pronouncedly.
Group G2: B cell proportion and number on D1 and B cell number on D7 decreased; B cell proportion on D7 and proportion and number on D11, D14, and D21 decreased more pronouncedly.
Compared to Group G2, Group G1 had lower B cell proportions and numbers on D11, D14, and D21, with a difference on D11.
T cell (TCRα/β+) proportion on D7, D14, and D21 increased.
No mice were euthanized due to welfare issues or unexpected death during the experiment.
Target
CD3 & CD19
Conjugated
Unconjugated
Application
ELISA, FACS, Functional assay
Chemical Information
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SMILES
[YK 012]
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)